Abstract: The invention concerns a method for preparing alkoxyamines in a biphasic medium. Said method consists in mixing an ionic liquid, an organic solvent, a metal salt, a metal ligand, a halogeno-carbonaceous ZX compound and a nitroxide, maintaining the reaction medium under agitation at a temperature between 20° C. and 90° C., until the nitroxide is eliminated, decanting, recuperating the organic phase, optionally washing it with water and then in isolating the alkoxyamine by evaporating the organic solvent under reduced pressure.

Abstract: The invention relates to a process for preparing alkoxyamines. This process consists in mixing, in an organic solvent, a metal salt, a ligand for the metal, a halocarbon compound ZX and a nitroxide, in keeping the reaction medium stirring at a temperature of between 20° C. and 90° C. until the nitroxide has disappeared, in recovering the organic phase, in washing it with water and then in isolating the alkoxyamine by evaporating the organic solvent under reduced pressure.

Abstract: A process for the production of an organic phosphorus-containing product, which comprises reacting a phosphorus-containing oxide with an unsaturated hydrocarbon in the presence of a boron-containing compound at a temperature of less than or equal to 50° C.

Abstract: An improved process is provided for preparing water-soluble prodrugs of triazole antifungal compounds containing a secondary or tertiary hydroxyl group. More particularly, the improved process is directed toward preparation of water-soluble triazole antifungal compounds are provided having the general formula wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and R and R1 are as defined in the specification.

Abstract: The present invention relates to novel cyclotriphosphazene derivatives represented by Formula (1) and a preparation method thereof wherein HNA is an amino acid group selected from glycine group(—NHCH2COO−), aminomalonic acid group(—NHCH(COO−)2), aspartic acid group (—NHCH(CH2COO−)COO−) and glutamic acid group (—NHCH(CH2CH2COO−)COO−), m is a repeating unit of poly(alkoxyethyleneglycol) selected from 2, 7, 12 and 16, and n is an integer representing number of alkyl carbons and selected from 0, 1, and 3.

Abstract: The present invention relates to an advantageous preparation of aryl compounds by cross-coupling reaction of a substituted aryl halide compound with a Grignard reagent in the presence of a nickel catalyst wherein the substituted aryl compounds and a novel nickel catalyst are initially placed in a reaction vessel and the Grignard reagent is metered in at the reaction temperature.

Abstract: Disclosed are novel bicyclic tris(anhydride)s useful as intermediates in the synthesis of biolologically active compounds, and the compounds which may be synthesized from such intermediates.

Abstract: This invention is directed to an improved process for the preparation of N-(phosphonomethyl)glycine (i.e., “glyphosate”), a salt of N-(phosphonomethyl)glycine, or an ester of N-(phosphonomethyl)glycine. The process comprises combining an N-substituted N-(phosphonomethyl)glycine reactant with oxygen in the presence of a noble metal catalyst.

Abstract: A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal alkoxide is reacted with a &bgr;-lactam.

Abstract: A method for the preparation of alkene phosphonic acids and salts thereof, such as VDPA (vinylidene diphosphonic acid) is disclosed. The products can be produced in a stable, substantially pure form and in high yield. The method includes the azeotropic removal of water from salts of &agr;-hydroxy-alkane diphosphonic acid dimer or corresponding acids thereof, and the pyrolysis of the dehydrated reactant at a temperature of from 170° C. to 300° C. There may be included a step to convert anhydrides which have been formed during the pyrolysis. The method may include the use of heat transfer agents and/or bases, and may be carried out at elevated or reduced pressure.

Abstract: A process for the preparation of a compound of formula I, ##STR1## wherein R.sup.1 and R.sup.2 are independently C.sub.1-6 alkyl, R.sup.3 is hydroxy and R.sup.4 and R.sup.5 are independently C.sub.1-6 alkyl is disclosed. The process comprises reacting a compound of formula II, ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are defined as in formula I and X is a leaving group, with a compound of formula III, ##STR3## wherein R.sup.4 and R.sup.5 are independently C.sub.1-6 alkyl, in the presence of a base.

Abstract: The present invention describes novel phosphonate reagent compositions of the formula: ##STR1## wherein R and R'=C.sub.1 -C.sub.4 alkyl groups, or R, R'=(CH.sub.2).sub.n (n=2 or 3) or [CH.sub.2 C(CH.sub.3).sub.2 CH.sub.2 ].The invention also describes allylic C-15 phosphonate compounds of the formula: ##STR2## wherein R and R'=C.sub.1 -C.sub.4 alkyl groups. The invention also describes methods of preparing phosphonate reagent compositions (4), allylic phosphonate compounds (5), and lycopene.

Abstract: The present invention describes novel C-15 allenic phosphonate reagent compositions of the formula: ##STR1## The invention also describes novel C-15 allylic phosphonate reagent compositions of the formula: ##STR2## The invention also describes methods of preparing canthaxanthin, the phosphonate reagent compositions, and a tertiary propargylic alcohol of the formula: ##STR3##

Abstract: A novel process for preparing aminomethylphosphonate derivatives involves the hydrogenation of cyanophosphonate derivatives in the presence of a catalyst to produce aminomethylphosphonate derivatives.

Abstract: The invention is relates to a method of producing aryl-substituted, amino-acylated phosphonic-acid derivatives with the aid of metal complexes of chiral amphiphilic ligands in that according to the invention .alpha.-N-acyl-protected, .beta.-substituted alkene phosphone derivatives are asymmetrically hydrogenated in the presence of a chiral rhodium catalyst in a solvent or a suspension. The use of the micelle-forming catalyst makes possible the hydrogenation of unsaturated phosphonic-acid derivatives in water with a high reaction rate with the obtainment of very good enantiomeric excesses.

Abstract: Aliphatic nitrate esters having a sulfur or phosphorus atom .beta. or .gamma. to a nitrate group and their congeners having efficacy as neuroprotective agents are described. Preferred nitrate esters may be synthesized by nitration of a 3-bromo-1,2-propanediol, and subsequent reaction to yield the desired mono-, di- or tetra-nitrate ester.

Abstract: A process for preparing cyanophosphonate derivatives involves contacting a phosphate ester and cyanide in a reaction mixture under conditions sufficient to produce a cyanophosphonate derivative. That cyanophosphonate derivative product can subsequently be hydrogenated to produce an aminomethylphosphonate derivative.

Abstract: A process for preparing cyanophosphonate derivatives involves contacting phosphoric anhydride (P.sub.4 O.sub.10) and a cyanide, preferably in the presence of a Lewis base, in a reaction mixture under sufficient conditions to produce a cyanophosphonate derivative. The cyanophosphonate derivative can be subsequently hydrogenated to produce an aminomethylphosphonate derivative.

Abstract: A process for preparing cyanophosphonate derivatives involves contacting a pyrophosphate ester or a polyphosphate ester and cyanide in a reaction mixture under conditions sufficient to produce the cyanophosphonate derivative. The cyanophosphonate derivative product can subsequently be hydrogenated to produce an aminomethylphosphonate derivative.

Abstract: Wittig-type reagents and methods of preparation and use thereof for preparing .alpha.,.beta.-unsaturated phosphonate esters from aldehydes and ketones are disclosed. The Wittig-type reagents have the following formulae: ##STR1## wherein X represents triflate, halide, BF.sub.4, SbF.sub.6, or ClO.sub.4 ; R.sub.1 represents alkyl, aryl or arylalkyl; and R.sub.2 represents alkyl, aryl or arylalkyl, provided that R.sub.1 and R.sub.2 not represent phenyl at the same time. The Wittig reagent diethyl phosphono-methylidenetriphenylphosphorane (1b) has been successfully synthesized for the first time via its phosphonium triflate salt (4a), by treating diethyl phosphonomethyltriflate with triphenylphosphine according to the disclosed method. The procedure has been applied to the synthesis of other new Wittig-type reagents such as phosphoranes and phosphonium salts. The new Wittig reagents thus synthesized were treated with various aldehydes and an activated ketone, affording the corresponding .alpha.,.beta.

Abstract: Compounds of formula (I), wherein Ar, R.sub.1, R.sub.2, Y and R are as defined in claim 1, are effective as traps for free radicals.

Abstract: Phosphites represented by the general formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.4 and R.sup.5 independently represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a cycloalkyl group having 5 to 8 carbon atoms, an alkylcycloalkyl group having 6 to 12 carbon atoms, an aralkyl group having 7 to 12 carbon atoms or a phenyl group; R.sup.3 and R.sup.6 independently represent a hydrogen atom or an alkyl group having 1 to 8 carbon atoms; X.sub.1 is a dihydric alcohol residue, wherein HO--X.sub.1 --OH defines the corresponding dihydric alcohol from which residue X.sub.1, is obtained; and X.sub.2 is a direct bond or an alkylene group having 1 to 8 carbon atoms; and the phosphites are useful as stabilizers for organic materials.

Abstract: This invention pertains to a synthetic process for obtaining a unique phosphocholine derivative which has been isolated from the leaves of the plant Irbachia alata, identified to be 1,22-bis?2-(trimethylammonium)ethylphosphatyl! docosane is disclosed. Also disclosed is a synthetic process for obtaining a novel class of mono- and bis(phosphocholine) derivatives which are useful as antiinfective agents. The compounds are particularly effective in treating fungal infections, especially those caused by Candida albicans, Cryptococcus neoformans, and Aspergillus fumigatus.

Abstract: A method of producing an ether-type thio-phospholipid of the formula (I): ##STR1## wherein: n is an integer of 13 to 17;A is C.sub.14 -C.sub.20 acyl group;G is a group selected from the group consisting of: ##STR2## which is useful as synthetic substrate of cytosolic phospholipase A.sub.2 inhibitors, said method being applicable to mass production of the compound (I), intermediates therefor and the preparation of the same are provided.

Abstract: A process for preparing an oxyglutaric acid ester derivative of the formula: ##STR1## in which each of R.sup.1 and R.sup.2 is C.sub.1-5 alkoxy, C.sub.1-7 aralkyloxy, C.sub.7-9 halogenated aralkyloxy or phenyl, R.sup.4 is a hydroxyl-protecting group, and R.sup.5 is C.sub.1-10 alkyl which may have a substituent, comprises the steps of reacting a methyl phosphonate derivative or methyl phosphine oxide derivative with an oxyglutaric acid mono-ester to give a reaction product which comprises an oxyglutaric acid derivative having a phosphorus-containing group and a pentenedioic acid mono-ester (by-product), removing the pendenedioic acid mono-ester from the reaction product to isolate the oxyglutaric acid derivative, and converting the isolated oxyglutaric acid derivative into the oxyglutaric acid ester derivative. A process for obtaining an optically active oxyglutaric acid ester derivative is also disclosed.

Abstract: The invention relates to a process for preparing phosphorus-containing compounds of the formula I ##STR1## in which R.sup.1 and R.sup.2 are an alkyl radical having 1 to 8 carbon atoms, a cyclohexyl radical, a cyclopentyl radical, an aryl radical or a halogen-, alkyl- or alkoxy-substituted aryl radical, where R.sup.1 and R.sup.2 together with the phosphorus atom can also form a ring, n and m=0 or 1 and R.sup.3 and R.sup.4 are alkyl radicals having 1 to 4 carbon atoms or n=0, m=0 or 1 and R.sup.3 and R.sup.4 are H, by adding compounds of the formula II ##STR2## into dialkyl esters of fumaric acid or of maleic acid of the formula (III) or dialkyl esters of itaconic acid of the formula (IV) ##STR3## in which R.sup.3 and R.sup.4 have the meaning given above, and, optionally reacting an alkyl ester of a phosphorus-containing dicarboxylic acid of the formula (I), where n=0, with water in the presence of catalytic amounts of an acid to give the phosphorus-containing dicarboxylic acid.

Abstract: This invention is selected novel chiral (essentially pure) alpha-amino phosphonates, process for the preparation which is a catalytic asymmetric hydrogenation of olefins and novel intermediates therefor. The alpha-amino phosphonates are useful as antibiotics and/or as intermediates in the preparation of phosphorus-containing analogs of peptides, i.e., phosphonopeptides or pseudopeptides having known uses, such as in antibiotics, antibiotic enhancers, or enzyme inhibitors.

Abstract: The addition of acid diesters of phosphorous acid onto alpha,beta-unsaturated carboxylic acid derivatives under basic catalysis is achieved with good yields if it is carried out in the presence of alkali metal alcoholates or phenolates and in the presence of halides, oxides or hydroxides of divalent metals. Co-use of these metal compounds allows relatively small mounts of metal alcoholates or phenolates to be used. The resulting reaction mixtures do not contain relatively large amounts of troublesome by-products.

Abstract: .alpha.-Phosphonosulfinate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2 is OR.sup.5 or R.sup.5a ; R.sup.3 and R.sup.5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R.sup.5a is alkyl, arylalkyl or aryl; R.sup.4 is H or a pharmaceutically acceptable cation; Z is H, halogen, lower alkyl or lower alkenyl; and R.sup.1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; including pharmaceutically acceptable salts.

Abstract: Compounds of the formula (I) in which: R is a possibly substituted amino group of the general form --NR.sub.1 R.sub.2, in which R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, lower alkenyl or lower alkinyl, or R is a saturated, unsaturated or aromatic heterocyclic ring which may be mono or bi-substituted by lower alkyl or halogen; alk is a valency bond, a methylene, a saturated or unsaturated, straight or branched-chain alkylene chain with 2-6 carbon atoms; and R.sup.3, R.sup.4, R.sup.5 are independently hydrogen, lower alkyl or benzyl; and their pharmacologically acceptable salts and enantiomers where, if R.sup.3 .dbd.R.sup.4 .dbd.R.sup.5 .dbd.CH.sub.3 and alk is a valency bond, R may not be the dimethyl amino group. Process for their production and medicaments containing these compounds, for the treatment of calcium metabolic complaints.

Abstract: The new amorphous modification of 1,1',1"-nitrilo{tri-2-propyl-tris-[2,2'-ethylidene-bis(4,6-di-tert-butylph enyl)]phosphite } is obtained by cooling rapidly said compound from the melt to ambient temperature.This amorphous form is an effective process stabilizer for polyolefins, particularly polypropylene.

Abstract: The new crystalline modification of 1,1',1"-nitrilo{tri-2-propyl-tris[2,2'-ethylidene-bis(4,6-di-tert-butylphe nyl)]phosphite} is obtained by crystallizing said compound from the melt at elevated temperatures.This crystalline form is an effective process stabilizer for polyolefins, particularly polypropylene.

Abstract: Heterosubstituted acetals of the formula ##STR1## can be obtained by reacting vinyl compounds of the formulaCH.sub.2 .dbd.CH-A.sup.1 (II)with alkyl nitrites of the formulaR.sup.1 --ONO (III.)The reaction is performed in the presence of palladium in metallic or bonded form and in alcohols or ethers as reaction medium at from 0.degree. to 120.degree. C.

Abstract: The present invention relates to catalytic asymmetric hydrogenation of phosphorus analogs of itaconic acid to synthesize novel optically active phosphono succinates.

Abstract: The present specification relates to an industrially advantageous process for producing vitamin A derivatives which are useful as medicaments, feed additives, food additives and the like. The process provides vitamin A derivatives, particularly all-trans vitamin A derivatives in high yield and purity.

Abstract: The present invention concerns nucleotide analogs and their compositions and use. In particular it relates to novel (phosphonomethoxy) methoxy purine/pyrimidine derivatives.

Abstract: Polyether bis-phosphonic acid compounds are disclosed which have the formula (HO).sub.2 OP--R--(OR').sub.n --OR--PO(OH).sub.2 where R is selected from the group consisting of methylene and ethylene, R' is selected from the group consisting of ethylene and ethylene substituted with one or more methyl groups, and n is an integer from 1 to 4, water soluble salts thereof, and esters thereof with alkyl groups having from 1 to 6 carbon atoms. Also disclosed is a novel preparation of these compounds by reacting hydroxyalkylphosphonic acid dialkyl ester compounds with 2-benzyloxyalkyl organic sulfonates; reacting the intermediate formed therefrom with hydrogen or a hydrogen source; reacting the intermediate formed therefrom with a hydrogen ion acceptor and certain sulfonyl chlorides; and reacting the intermediate formed therefrom with hydroxyalkylphosphonic acid dialkyl ester compounds to form a polyether bis-phosphonic acid compound which may be hydrolyzed to form the polyether bis-phosphonic acid.

Abstract: Disclosed herein are phosphoric acid esters of myoinositol, which are represented by the following general formula (I): ##STR1## and their salts, as well as a preparation process thereof. The myoinositol derivatives can each be obtained by causing a phosphorylating agent to act on a myoinositol derivative substituted with catalytic reduction removable substituent groups at the positions other than those desired to be substituted by phosphoric acid residual groups and then catalytically reducing the thus-phosphorylated myoinositol.

Abstract: A process for the preparation of diesters of carboxymethylphosphonic acid of the formula: (RO).sub.2 P(O)CH.sub.2 CO.sub.2 H, in which R is a straight-chain or branched alkyl radical having 1 to 20 carbon atoms, a cycloaliphatic radical having 5 to 8 carbon atoms, a phenyl or naphthyl radical which can be substituted, an aralkyl radical having 7 to 10 carbon atoms, or in which the (RO).sub.2 P group forms a ring having 2 to 5 carbon atoms which can be substituted, characterized in that dialkyl ester of 2-hydroxyethylphosphonic acid of the formula (RO).sub.2 P(O)CH.sub.2 CH.sub.2 OH, in which R has the abovementioned meaning, is reacted with oxygen in the presence of water and a catalyst which contains at least one metal selected from the platinum metals group.

Abstract: Methods for converting phosphonates into thiophosphonates and specific thiophosphonate compounds so produced are disclosed and claimed. The methods start with a reaction mixture formed of a phosphonate compound, including one or more strong electron-withdrawing groups located adjacent to the phosphorus in the compound, a slight excess of Lawesson's reagent, and a polar aprotic solvent. The reaction mixture is heated until reaction is complete and may be followed with separation or hydrolyzation steps to produce thiophosphonic acids and their addition salts. One of these thio-analogues, thiophosphonoformic acid (TPFA) is particularly effective at inhibiting HIV replication and in treating HIV infection.

Abstract: New chemical product, constituted by an organic phosphorus compound of the structure ##STR1## where Q is an N or O atom, T is an alkylene or arylene, possibly carrying substituents, or not existing, while R.sup.1 to R.sup.7, the same or different, are H or aliphatic, cycloaliphatic and/or arylic hydrocarbon radicals, possibly substituted, R.sup.3 not existing when Q is oxygen. This product is used as an intermediate in the preparation of different derivatives of phosphinous acid.

Abstract: In order to prepare N-acylphosphinothricin diesters, acetals of methyl-(3-oxopropyl)phosphinic acid esters of the formula ##STR1## are reacted in a dipolar aprotic solvent with a carboxylic acid amide and carbon monoxide in the presence of hydrogen gas using a cobalt compound as a catalyst, where the radical R' is alkyl or aryl or aralkyl.

Abstract: Processes for synthesizing novel phosphonate diester compounds of the general formula ##STR1## are disclosed and claimed. The claimed process includes forming a reaction mixture of a C-14 aldehyde and a methylene-bis-phosphonic acid ester, separating a pentadienyl phosphonic acid dialkyl ester intermediate from the reaction mixture, optionally isomerizing the intermediate in the presence of a basic catalyst, and isolating the desired pentadienylphosphonic acid dialkyl ester compound. The isolated phosphonate compounds made according to the processes of the present invention may be employed in synthesizing retinoids such as retinoic acid or carotenoids such as beta-carotene.

Abstract: Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, or wherein R denotes methyl, R.sub.1 denotes hydrogen or hydroxy, R.sub.2 denotes an aromatic radical and R.sub.3 represents hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.

Abstract: A process for preparing surface-active, saturated sulfophosphoric acid-(partial)-alkyl esters and their alkali metal, alkaline earth, ammonium and/or amine salts by the sulfonation of saturated phosphoric acid-(partial)-alkyl esters and then hydrolysis of the sulfonated phosphoric acid esters formed.

Abstract: Novel phosphonate compounds of the formula ##STR1## are disclosed and claimed, as well as methods for manufacturing the phosphonates from C-14 through C-16 aldehydes. The phosphonate compounds of the present invention can be employed to form 13-cis retinoic acid, retin-A and beta-carotene.

Abstract: A process for producing a phosphinylamino acid derivative of the formula: ##STR1## wherein R.sup.1 is a lower alkyl group, R.sup.2 is a hydrogen atom, a lower alkyl group, a halo-lower alkyl group or a substituted or unsubstituted phenyl group, and R.sup.3 is a substituted or unsubstituted alkyl group or a substituted or unsubstituted phenyl group, which comprises reacting a compound of the formula: ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, and/or a compound of the formula: ##STR3## wherein R.sup.1 and R.sup.2 are as defined above, with a compound of the formula:R.sup.3 CONH.sub.2 (IV)wherein R.sup.3 is as defined above, carbon monoxide and hydrogen in the presence of a catalyst containing a metal of group VIII of the Periodic Table.

Abstract: A process is provided for preparing phosphonyloxyacylamino acids and derivatives thereof having the structure ##STR1## wherein X is ##STR2## which includes the steps of treating a phosphonic acid dichloride of the structure ##STR3## with an .alpha.-hydroxy acid of the structure ##STR4## in the presence of base such as triethylamine at reduced temperatures to form the cyclic mixed anhydride of the structure ##STR5## (which is a new intermediate) and reacting the cyclic mixed anhydride with an amino acid or ester of the structureHXin the presence of base such as triethylamine produces the ACE inhibitor compound ##STR6## In an alternative process, the cyclic anhydride is quenched with water to form the diacid ##STR7## which is treated with a condensing agent such as dicyclohexyl carbodiimide (DCC), 1,1-carbonyldiimidazole (CDI) or thionyl chloride followed by quenching with the amino acidHXproduces the above ACE inhibitor compound.

Abstract: Preparation of intermediates for herbicides of formula ##STR1## by the reaction of organic phosphites with benzoxazines of formulaBzx--CH.sub.2 --CO--Y (II)in whichBzx denotes the radical of formula: ##STR2## X is a usual substituent of phenols n is an integer from 0 to 4R.sup.1 and R.sup.2 are H or such that OR.sup.1 and OR.sup.2 are hydrolyzableY is --OM or --NR.sup.3 R.sup.4M is H or is such that COOM is a salt or an esterR.sup.3 and R.sup.4 are H or a hydrocarbon radical, and one of them can be R.sup.5 --SO.sub.2 --, andR.sup.5 is a hydrocarbon radical, substiuted if appropriate. Products obtained by the process and their use as herbicides.