Abstract: The present invention provides a process that enables a substituted methylamine compound which is useful as an intermediate for the production of agricultural chemicals and medicines, to be produced easily, with good yield, and at low cost, and also provides a production intermediate thereof. The process comprises a step of reacting a hexamethylenetetraammonium salt compound represented by a formula (I) with a base to obtain an N-methylidene-substituted methylamine oligomer represented by a formula (II) or a mixture of two or more of the oligomers, and a step of hydrolyzing the N-methylidene-substituted methylamine oligomer represented by formula (II) or the mixture of two or more of the oligomers in the presence of an acid. (wherein A represents an organic group, R represents a hydrogen atom, or an organic group, L represents a halogen atom and the like, and n represents an integer of 2 to 20).

Abstract: The present invention provides a process for effectively producing an N-(hetero)arylazole with high yield, which is useful as a medical or agrochemical product, an organic photoconductor material, an organic electroluminescent element material, or the like. The present invention relates to a process for producing an N-(hetero)arylazole, which includes reacting a (hetero)aryl (pseudo)halide with an NH-azole in the presence of: a catalyst including a palladium compound and a coordination compound; and a basic magnesium compound.

Abstract: The present invention relates to an improved process for preparation of Dasatinib monohydrate Formula A, comprising the steps of: a) reacting the compound of Formula I with 1-(2-Hydroxyethyl)piperazine (Formula II) in the presence of acetonitrile solvent, an organic base and a phase transfer catalyst; b) heating the reaction mixture at 50-80° C.; c) adding water to the reaction mass obtained in step b); d) cooling the reaction mixture to a temperature below 35° C.; e) filtering and drying the material obtained in step d); f) optionally purifying the product obtained from step e); g) isolating the crystalline Dasatinib monohydrate.

Abstract: The present invention provides novel ruthenium based catalysts, and a process for preparing amines, by reacting a primary alcohol and ammonia in the presence of such catalysts, to generate the amine and water. According to the process of the invention, primary alcohols react directly with ammonia to produce primary amines and water in high yields and high turnover numbers. This reaction is catalyzed by novel ruthenium complexes, which are preferably composed of quinolinyl or acridinyl based pincer ligands.

Abstract: A process is described for preparing aromatic and heteroaromatic amines of the general formula (I) Ar—NR1R2, in which an aromatic compound with the general formula (II) Ar—X is reacted in the presence of a catalyst with an amine of the general formula (III) H—NR1R2 and a base, wherein the catalyst is selected from transition metal complexes having one or more ligands with the general formula (IV).

Abstract: Process for preparing 2,2-difluoroethylamine, comprising the following steps: (i) mixing 2,2-difluoro-1-chloroethane and gaseous, liquid or supercritical ammonia in a pressure-stable, closed reaction vessel under a pressure in the range from 10 to 180 bar; (ii) reacting the reaction mixture at a reaction temperature in the range from 80° C. to 200° C.; (iii) letting down the reaction mixture and isolating 2,2-difluoroethylamine.

Abstract: An improved method for the synthesis of substituted formylamines and substituted amines via an accelerated Leuckart reaction. The Leuckart reaction is accelerated by reacting formamide or N-alkylformamide and formic acid with an aldehyde or a ketone at a preferred molar ratio that accelerates the reaction. The improved method is applicable to various substituted aldehydes and ketones, including substituted benzaldehydes. An accelerated method for the hydrolysis of substituted formylamines into substituted amines using acid or base and a solvent at an elevated temperature. The improved method is useful for the accelerated synthesis of agrochemicals and pharmaceuticals such as vanillylamine, amphetamine and its analogs, and formamide fungicides.

Abstract: [Problem] The present invention aims to provide a novel organometallic compound that can be used as a general-use highly active catalyst with superior selectivity for functional groups. [Means for Solving Problem] The present invention relates to an organometallic compound having a novel specific structure of general formula (1): and to a general-use highly active catalyst used in reductive amination reaction with superior selectivity for functional groups that comprises said organometallic compound, and to a process for preparing amine compounds by reductive amination reaction using said catalyst.

Abstract: Process for the preparation of 2,2-difluoroethylamine of the formula (I) CHF2CH2NH2??(I) comprising the stages (i) and (ii): stage (i): reaction of 2,2-difluoro-1-haloethane of the general formula (II) CHF2—CH2Hal??(II), with a benzylamine compound of the formula (III) in the presence of an acid scavenger, in which, in formula (II), Hal is chlorine, bromine or iodine, and, in the formulae (III), R1 is hydrogen or C1-C12-alkyl, and R2 is hydrogen, halogen, C1-C12-alkyl or C1-C6-alkoxy; stage (ii): catalytic hydrogenation of the N-benzyl-2,2-difluoroethanamine compound obtained in the stage (i) to give 2,2-difluoroethylamine of the formula (I) or a salt thereof.

Abstract: An improved method for the synthesis of substituted formylamines and substituted amines via an accelerated Leuckart reaction. The Leuckart reaction is accelerated by reacting formamide or N-alkylformamide and formic acid with an aldehyde or a ketone at a preferred molar ratio that accelerates the reaction. The improved method is applicable to various substituted aldehydes and ketones, including substituted benzaldehydes. An accelerated method for the hydrolysis of substituted formylamines into substituted amines using acid or base and a solvent at an elevated temperature. The improved method is useful for the accelerated synthesis of agrochemicals and pharmaceuticals such as vanillylamine, amphetamine and its analogs, and formamide fungicides.

Abstract: Disclosed is a method for producing a primary amine compound represented by the formula (3): wherein, Ar is as defined below, which is characterized in that a halogen compound represented by the formula (1): wherein, Ar represents an unsubstituted aromatic group such as a phenyl group, a naphthyl group, a pyridyl group, a furyl group, a thienyl group, a pyrrolyl group, an oxazolyl group, an isoxazolyl group or a pyrimidinyl group, or an aromatic group obtained by substituting such an unsubstituted aromatic group with 1-3 substituents; and X represents a halogen atom, ammonia and formaldehyde are reacted with each other, thereby obtaining a hexahydrotriazine compound represented by the formula (2): wherein, Ar is as defined above, and then the thus-obtained hexahydrotriazine compound is decomposed. By this method, a primary amine compound can be commercially advantageously produced by using a low-cost ammonia while suppressing production of a secondary amine as a by-product.

Abstract: Process for the preparation of 2,2-difluoroethylamine of the formula (I) CHF2CH2NH2??(I) comprising the stages (i) and (ii): stage (i): reaction of 2,2-difluoro-1-haloethane of the general formula (II) CHF2—CH2Hal??(II), with a benzylamine compound of the formula (III) in the presence of an acid scavenger, in which, in formula (II), Hal is chlorine, bromine or iodine, and, in the formulae (III), R1 is hydrogen or C1-C12-alkyl, and R2 is hydrogen, halogen, C1-C12-alkyl or C1-C6-alkoxy; stage (ii): catalytic hydrogenation of the N-benzyl-2,2-difluoroethanamine compound obtained in the stage (i) to give 2,2-difluoroethylamine of the formula (I) or a salt thereof.

Abstract: The present invention provides novel ruthenium based catalysts, and a process for preparing amines, by reacting a primary alcohol and ammonia in the presence of such catalysts, to generate the amine and water. According to the process of the invention, primary alcohols react directly with ammonia to produce primary amines and water in high yields and high turnover numbers. This reaction is catalyzed by novel ruthenium complexes, which are preferably composed of quinolinyl or acridinyl based pincer ligands.

Abstract: Disclosed is a method for producing a primary amine compound represented by the formula (3): wherein, Ar is as defined below , which is characterized in that a halogen compound represented by the formula (1): wherein, Ar represents an unsubstituted aromatic group such as a phenyl group, a naphthyl group, a pyridyl group, a furyl group, a thienyl group, a pyrrolyl group, an oxazolyl group, an isoxazolyl group or a pyrimidinyl group, or an aromatic group obtained by substituting such an unsubstituted aromatic group with 1-3 substituents; and X represents a halogen atom, ammonia and formaldehyde are reacted with each other, thereby obtaining a hexahydrotriazine compound represented by the formula (2): wherein, Ar is as defined above, and then the thus-obtained hexahydrotriazine compound is decomposed. By this method, a primary amine compound can be commercially advantageously produced by using a low-cost ammonia while suppressing production of a secondary amine as a by-product.

Abstract: The present invention relates to a method of producing an optically active 1-aryl-2-fluoro-substituted ethylamine compound of the formula [2] or a salt thereof by hydrogenolysis of an optically active secondary amine compound of the formula [1] or a salt thereof in the presence of a transition metal catalyst of Group VIII [Chem. 59] [where Ar represents an aryl group; n represents an integer of 1 or 2; and * represents an asymmetric carbon] [Chem. 60] [where Ar represents an aryl group; n represents an integer of 1 or 2; and * represents an asymmetric carbon].

Abstract: A method of synthesizing a compound of formula I: comprising the step of reacting a moiety of formula II: with a moiety of formula III: in compressed carbon dioxide in the presence of a transition metal catalyst and a base, wherein L is a labile leaving group; RN1 is optionally substituted C5-20 aryl; RN2 is selected from optionally substituted C5-20aryl, optionally substituted C3-20 heterocyclyl, optionally substituted C3-7 alkyl, and optionally substituted sulfonyl; RN3 is selected from H and optionally substituted C1-7 alkyl, C3-20 heterocyclyl and C5-20 aryl; or RN2 and RN3 together with the nitrogen atom to which they are attached form optionally substituted nitrogen-containing C3-20 heterocylyl or C5-20 heteroaryl; and R1 R2 and R3 are independently selected from optionally substituted C1-7 alkyl, C5-20 aryl, C3-20 heterocyclyl, hydroxy, halo, amino and C1-7 alkoxy, or two of R1, R2 and R3, together with the silicon atom to which they are attached, may form a silicon containing C5-7 heterocyclyl group.

Abstract: There are provided novel compounds of formula (I) wherein A, R1, R3, R4, R5, T, U, V, W, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy.

Abstract: The invention concerns phosphorus-containing dendrimers and their uses, as gene transfection agents, in vitro and in vivo, including in the treatment of human and animal diseases. These agents or vectors are in particular suited for delivering to appropriate target cells, nucleic acid sequences of interest.

Abstract: This invention discloses a rubbery polymer which is comprised of repeat units that are derived from (1) at least one conjugated diolefin monomer, and (2) at least one functionalized monomer having of the structural formula: wherein R represents an alkyl group containing from 1 to about 10 carbon atoms or a hydrogen atom, and wherein R1 and R2 can be the same or different and represent hydrogen atoms or a moiety selected from the group consisting of wherein R3 groups can be the same or different and represent alkyl groups containing from 1 to about 10 carbon atoms, aryl groups, allyl groups, and alkyloxy groups of the structural formula —(CH2)y—O—(CH2)z—CH3, wherein Z represents a nitrogen containing heterocyclic compound, wherein R4 represents a member selected from the group consisting of alkyl groups containing from 1 to about 10 carbon atoms, aryl groups, and allyl groups, and wherein n, x, y and z represents integers from 1 to about 10, with the

Abstract: The antifungal agent (E)-N-methyl-N-(1-naphthylmethyl)-6,6-dimethyl-hept-2-ene-4-ynyl-1-amine of formula (I) and acid addition salts thereof are prepared by reacting a chloro-compound of formula (IIIb) with a secondary amine of formula (II) in an aliphatic ketone-type solvent in the presence of a base and optionally iodide salt catalyst, and subsequently treating the resulting reaction mixture directly with aqueous hydrochloric acid to precipitate the hydrochloride of the compound of formula (I). The precipitate is separated, and the base of formula (I) can be liberated from the hydrochloride and can be converted into other pharmaceutically acceptable acid addition salts.

Abstract: The present invention relates to a novel antiozonant as well as antioxidant based on functionalized hindered phenol and the process for the preparation thereof of formula 1 wherein R1 is tert-butyl and R2 and R3 are C1 to C8 linear or branched alkyl. The present invention also relates to a process for the preparation thereof comprising dissolving a compound of formula 3 wherein R1 is tert-butyl, with liquid bromine in a non polar organic solvent at temperature range 80 to 95° C. for a period of 4 to 7 hours, evaporating the solvent under reduced pressure to obtain a compound of formula 2 wherein R1 is a tertiary butyl group and X is Br, reacting the compound of formula 2 with a compound of formula 4 wherein R2 and R3 are C1 to C8 linear or branched alkyl, dissolved in an organic solvent in presence of a suitable mild base at a temperature ranging from 80 to 95° C.

Abstract: The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate.

Abstract: The present invention relates to a process for hydrolyzing optically active amides to carboxylic acids and optically active amines with retention of the center of chirality, where the hydrolysis of the amides is carried out with an alkali metal or alkaline earth metal hydroxide in the presence of 5-30% by weight, based on the amide employed, of a polyol or an amino alcohol.

Abstract: Novel N-substituted-aminomethyl cyclopropyl ketone derivatives are represented by following Formula (1): wherein R1, R2 and R3 are each a hydrogen atom or an aliphatic hydrocarbon group; and R4 and R5 are each a hydrogen atom or an arylmethyl group which may have a substituent, where at least one hydrogen atom or aryl group as a substituent is combined with a carbon atom in the methyl moiety of the arylmethyl group, and at least one of R4 and R5 is an arylmethyl group which may have a substituent. These compounds are useful for the preparation of aminomethyl cyclopropyl ketone derivatives and 2-amino-1-cyclopropylethanol derivatives or salts thereof.

Abstract: This invention discloses a rubbery polymer which is comprised of repeat units that are derived from (1) at least one conjugated diolefin monomer, and (2) at least one functionalized monomer having of the structural formula: wherein R represents an alkyl group containing from 1 to about 10 carbon atoms or a hydrogen atom, and wherein R1 and R2 can be the same or different and represent hydrogen atoms or a moiety selected from the group consisting of wherein R3 groups can be the same or different and represent alkyl groups containing from 1 to about 10 carbon atoms, aryl groups, allyl groups, and alkyloxy groups of the structural formula —(CH2)y—O—(CH2)z—CH3, wherein Z represents a nitrogen containing heterocyclic compound, wherein R4 represents a member selected from the group, consisting of alkyl groups containing from 1 to about 10 carbon atoms, aryl groups, and allyl groups, and wherein n, x, y and z represents integers from 1 to about 10, with the

Abstract: N-Benzylamines are prepared by a process in which (i) in a first step, a benzaldehyde is reacted with a primary amine to give the imine and (ii) in a second step, the imine is hydrogenated with hydrogen in the presence of a catalyst containing one or more metals of groups 8 to 10 of the Periodic Table of the Elements to give the N-benzylamine, wherein the iminization (i) is carried out in a water-miscible solvent and the resulting water of reaction is not removed, and the hydrogenation (ii) is carried out in the imine solution obtained in the iminization (i) and containing water of reaction.

Abstract: A method is provided for the transition metal-catalyzed arylation, or vinylation, of hydrazines, hydrazones, and the like. Additionally, the invention provides a conceptually novel strategy, the cornerstone of which is the transition metal-catalyzed arylation or vinylation method, for the synthesis of indoles, carbazoles, and the like. The methods and strategies of the invention may be utilized in standard, parallel, and combinatorial synthetic protocols.

Abstract: A method for selective mono-N-alkylation of primary amines to produce secondary amines that are substantially free of overalkylated tertiary amines and quaternary ammonium salts, under mild reaction conditions without the necessity of protecting groups. Compounds of the class of secondary amines are produced by reacting an alkyl halide with an alkyl amine in anhydrous solvent, preferably dimethyl sulfoxide or N,N-dimethylformamide, in the presence of 0.1 to 3 molar equivalents of a cesium base. Optionally, the extent and selectivity of mono-N-alkylation is enhanced by addition to the reaction mixture of a powdered molecular sieve material for removal of water produced by the reaction, and/or tetrabutylammonium iodide to promote halide exchange. The invention permits selective and efficient mono-N-alkylation of a wide variety of substrates at 23° C.

Abstract: A method is provided for the transition metal-catalyzed arylation, or vinylation, of hydrazines, hydrazones, and the like. Additionally, the invention provides a conceptually novel strategy, the cornerstone of which is the transition metal-catalyzed arylation or vinylation method, for the synthesis of indoles, carbazoles, and the like. The methods and strategies of the invention may be utilized in standard, parallel, and combinatorial synthetic protocols.

Abstract: The transition metal-catalyzed amination of aryl halides, in conjunction with an orthogonal protective group scheme, forms the basis of two routes to oligoaniline precursors. The oligoaniline precursors are soluble in a variety of common organic solvents, and are easily converted to the deprotected oligoanilines. The method allows the preparation of oligoanilines of even or odd chain lengths, and the incorporation of a variety of functional groups into the oligomers. Polyanilines of low polydispersity can also be prepared by this method.

Abstract: The invention is a process to manufacture the intermediate secondary amine N-ethyl-2-chloro-6-fluoro-benzylamine, and then the process of reacting this intermediate to manufacture the herbicide flumetralin. Equimolar quantities of monoethylamine, sodium hydroxide, and 2-chloro-6-fluorobenzyl chloride are reacted at a temperature between about 70.degree. C. and about 100.degree. C. in a composition containing at least 2.5 times the required quantity of monoethylamine. The reagent monoethylamine functions as solvent and heat sink for the reaction, and also minimizes the formation of undesired byproducts. The excess monoethylamine is removed after formation of the intermediate. Then, equimolar quantities of sodium hydroxide in water and molten 4-chloro-3-5-dinitrobenzotrifluoride are added to the intermediate, and the temperature is controlled between about 90.degree. C. and about 115.degree. C. The product of this reaction is relatively pure, i.e., 98 percent by weight, molten flumetralin.

Abstract: Disclosed is a process for the preparation of N-aryl amine compounds, comprising reacting an amine compound with an arylating compound in the presence of a base and a transition metal catalyst under reaction conditions effective to form an N-aryl amine compound, the transition metal catalyst comprising a Group 8 metal and P(t-Bu).sub.3 as a ligand, and wherein the ratio of the ligand to the Group 8 metal is in the range of about 3:1 to about 0.25:1, and wherein the reaction temperature is less than 100.degree. C. The process of the present invention provides a useful general method of N-arylation for the manufacture of pharmaceuticals, polymers, and the like.

Abstract: The method of the present invention provides a simple general route to a wide range of secondary amines.

Abstract: Novel aminomethylphosphine ligands have particular substituents on the central carbon atom. Such ligands form coordination complexes that may be catalysts for the polymerization of monomers or other catalytic induced reactions.

Abstract: A heterocyclic aromatic halide or an aryl halide is reacted with an amine compound in the presence of a base to give a heterocyclic aromatic amine or an arylamine, respectively. In this reaction, a catalyst comprising a palladium compound and a tertiary phosphine is used for the preparation of a heterocyclic aromatic amine, and a catalyst comprising a palladium compound and a trialkylphosphine is used for the preparation of an arylamine.

Abstract: A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide or cyanohydrin from a chiral alpha amino aldehyde.

Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.

Abstract: The present invention relates to a process for preparing protected amines or amino acids. The invention furthermore relates to the use of tocopheryl radicals or radicals derived therefrom as protective groups for amines and amino acids, and to compounds obtained in this process as intermediates and to processes for preparing dipeptides and oligopeptides.

Abstract: A method of preparing an arylamine compound includes reacting a metal amide comprising a metal selected from the group consisting of tin, boron, zinc, magnesium, indium and silicon, with an aromatic compound comprising an activated substituent in the presence of a transition metal catalyst to form an arylamine. The method is useful in preparing mixtures of arylamines for use in screening for pharmaceutical and biological activity and in preparing poly(anilines).

Abstract: A benzylamine derivative or salt thereof having antidepressant and antianxiety activities having the general formula: ##STR1## wherein R.sup.1 is a lower alkyl group;R.sup.2 is a cycloalkyl group; andR.sup.3 is a halogen atom;or salt thereof.

Abstract: A process for the preparation of arylbenzylamines by the reaction of arylamines with a benzyl chloride, wherein the reaction is carried out in the presence of both a phase-transfer catalyst and a base selected from the group consisting of the inorganic bases and salts of weak organic acids.

Abstract: A compound of the formula: ##STR1## wherein R.sup.11 is hydrogen, lower alkyl, haloloweralkyl, lower alkenyl, lower alkynyl or cycloalkyl and R.sup.21 is a group selected from the group consisting of: ##STR2## wherein R.sup.3 -R.sup.5, R.sup.31, R.sup.32, R.sup.41, R.sup.42 and R.sup.51 are as defined herein, and W is chlorine or bromine, is prepared by reacting a compound of the formula:Z--CH.sub.2 --CH.dbd.CH--W (I)wherein W is as defined above and Z is a leaving group, with an amine of the formula: ##STR3## wherein R.sup.11 and R.sup.21 are as defined above.

Abstract: N-benzyl-N-organo-substituted aminoalkanol is prepared by reacting benzyl chloride or substituted benzyl chloride with an organo-substituted aminoalkanol in the presence of a molar excess of the starting aminoalkanol and, optionally, water, and in the absence of a) an organic solvent for the reactants and b) alkali metal hydroxide. A portion of the excess aminoalkanol may be substituted with an alternative amine or dissolved alkali metal carbonate.

Abstract: A process for producing an enyne derivative, and intermediate, which is useful for preparing compounds showing strong inhibiting activities against squalane.epoxidase of Eumycetes and strong anti-cholesterol activities. The process comprises reacting a compound of the formula:Z--CH.sub.2 --CH.dbd.CH--W [I]wherein W is a halogen atom, and Z is a leaving group, with an amine in the presence of a base, if necessary, to obtain a compound of the formula: ##STR1## then reacting an acetylene derivative to this compound in the presence of a palladium catalyst, to obtain a compound of the formula: ##STR2## and, if necessary, N-alkylating this compound.

Abstract: A process for producing a benzylamine which comprises reacting a benzyl halide with an aqueous ammonia solution in the presence of an aromatic aldehyde represented by the formula: ##STR1## wherein R represents a hydrogen atom, a halogen atom or a lower alkyl group, and n is 1 or 2, separating an oily substance from the reaction mixture, and treating the oily substance with a mineral acid.

Abstract: An optically active amine compound and a method for preparing same are provided which compound has the structure ##STR1## in the form of its R-(+) enantiomer or S-(-) enantiomer, wherein R and R.sup.1 are independently H, lower alkyl or halogen, R.sup.2 is H or lower alkyl and R.sup.3 is lower alkyl, the optically active amine is useful in the optical resolution of DL-3-acylthio-2-methylpropanoic acid wherein acyl is acetyl or benzoyl. The optically active D-(+)-3-acylthio-2-methylpropanoic acids are used as intermediated for preparing antihypertensive agents, such as captopril.

Abstract: A process is disclosed for preparing bidentate ligands of the formula: ##STR1## wherein: each Ar is independently selected from aromatic ring compounds having 6 up to 14 carbon atoms, e.g., phenyl, naphthyl, phenanthryl and anthracenyl;the x bonds and the y bonds are attached to adjacent carbon atoms on the ring structures;each R, when present as a substituent, is independently selected from alkyl, alkoxy, aryloxy, aryl, aralyky, alkaryl, alkoxyalky, cycloaliphatic, halogen, alkanoyl, alkanoyloxy, alkoxycarbonyl, carboxyl, cyano or formyl radicals;n is a whole number in the range of 0-4 where Ar is phenyl; 0-6 where Ar is naphthyl; and 0-8 where Ar is phenanthryl or anthracenyl;each R.sub.1 and R.sub.2 is independently selected from alkyl, aryl, aralkyl, alkaryl or cycloaliphatic radicals, or substituted derivatieves thereof;each R.sub.3 and R.sub.4 is independently selected from hydrogen and the R.sub.

Abstract: A process is disclosed for preparing bidentate ligands of the formula: ##STR1## wherein: each AR is independently selected from aromatic ring compounds having 6 up to 14 carbon atoms, e.g., phenyl, naphthyl, phenanthryl and anthracenyl;the x bonds and the y bonds are attached to adjacent carbon atoms on the ring structures;each R, when present as a substituent, is independently selected from alkyl, alkoxy, aryloxy, aryl, aralkyl, alkaryl, alkoxyalkyl, cycloaliphatic, halogen, alkanoyl, alkanoyloxy, alkoxycarbonyl, carboxyl, cyano or formyl radicals;n is a whole number in the range of 0-4 were Ar is phenyl; 0-6 where Ar is naphthyl; and 0-8 where Ar is phenanthryl or anthracenyl;each R.sub.1 and R.sub.2 is independently selected from alkyl, aryl, aralkyl, alkaryl or cycloaliphatic radicals, or substituted derivatives thereof;each R.sub.3 and R.sub.4 is independently selected from hydrogen and the R.sub.

Abstract: An allyl type amine is prepared by reacting an allyl type alcohol represented by the following formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 independently stand for a hydrogen atom, an aliphatic hydrocarbon group or alicyclic hydrocarbon having 1 to 8 carbon atoms, or an aromatic hydrocarbon group,with at least one member selected from the group consisting of ammonia, a primary amine and a secondary amine in the presence of a palladium compound and a multidentate phosphorus compound.

Abstract: Disclosed is a novel inosose compound represented by the general formula: ##STR1## wherein X.sup.1 and X.sup.2 are both halogen; X.sup.1 is hydrogen and X.sup.2 is halogen; or X.sup.1 is --SQ.sup.1 and X.sup.2 is --SQ.sup.2 (each of Q.sup.1 and Q.sup.2 is lower alkyl or Q.sup.1 and Q.sup.2 may form lower alkylene), R.sup.1 is a protective group for hydroxyl and Y is .dbd.O, .dbd.N--Z (Z is hydroxyl which may be protected) or ##STR2## (A is hydrogen or an amine residue), particularly to the compound wherein the symbol Y is oxygen.The inosose compound is useful as intermediates for production of valiolamine and the N-substituted derivatives thereof, which have potent .alpha.-glucosidase inhibiting activities and are useful as preventives or therapeutics for symptoms of hyperglycemia and various diseases derived therefrom in human and animals, such as diabetes, obesity and hyperlipemia.