Abstract: Sterically hindered phosphoramidates such as N,N′-bis[di-(2,6-xylenoxy)phosphoryl]piperazine are prepared by the reaction of a sterically hindered diaryl chlorophosphate, such as di-(2,6-xylyl) chlorophosphate, with a basic nitrogen compound containing at least two basic N-H groups, preferably a heterocyclic compound such as piperazine, in the presence of calcium oxide as an acid acceptor. The reaction is conducted in the presence of at least one dipolar aprotic solvent.

Abstract: Compounds of Formula I are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathsepsin D. The compounds are useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is a heterocycle, amide, sulfonamide or carbamate and Z is an acyl or a functionalized acyl. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid phase support, are also disclosed.

Abstract: The present invention provides novel, water-soluble, red-emitting fluorescent rhodamine dyes and red-emitting fluorescent energy-transfer dye pairs, as well as labeled conjugates comprising the same and methods for their use. The dyes, energy-transfer dye pairs and labeled conjugates are useful in a variety of aqueous-based applications, particularly in assays involving staining of cells, protein binding, and/or analysis of nucleic acids, such as hybridization assays and nucleic acid sequencing.

Abstract: The invention relates to novel dipyrano-quinolinone class of compounds having the general formula: Wherein R is hydrogen, alkyl optionally substituted about C-1 to C-10 alkenyl optionally substituted about C-1 to C-10 with one or more double bounds, alkynyl optionally substituted about C-1 to C-10 with one or more triple bonds, aryl, hetero aryl, carbocyclic aryl, alkyl aryl, alcyclic compounds, C-1 to C-6 alkyl with terminal dialkyl amino group, thio alkyl, hydroxyl alkyl groups; R1 is H, lower dialkyl amino alkyls such as methyl, ethyl, propyl, and other alkyl groups or b-amino acid moieties, hydroxy alkyl groups having optionally substituted about C-1 to C-10 carbons, acid amides such as aliphatic acids, aromatic acids, sulphonic acids trihalo acids.

Abstract: A process for preparing thiopyridines of the formula I where the substituents are as defined in the description.

Abstract: Disclosed are crystals of a compound represented by the formula: and processes for preparing them.

Abstract: 5-Membered ring heterocycle of the formula I, in which D includes a COOR15, CON(CH3)R15 or CONHR15 radical and R15 includes a 6-24 member bicyclic or tricyclic radical, compositions, preparation and use as inhibitors of thrombocyte aggregation, metastasization of carcinoma cells, binding of osteoclasts to bone surfaces and for the treatment of tromboses.

Abstract: Pyrazole intermediates in a method for the preparation of &bgr;-amino acid compounds are provided. The method includes contacting an amine nucleophile with an &agr;,&bgr;-unsaturated amide compound in the presence of a chiral Lewis acid complex. The chiral Lewis acid complex is formed from an azophilic metal salt and a chiral bisoxazolinylmethane compound. The selective amidolysis of one enantiomer of the &bgr;-aminoamide product is also described.

Abstract: A ferroceneylphosphine ligand and complexes prepared therefrom for homogeneous catalytic enantioselective hydrogenation, the ligand having the formula (I): Another aspect of the invention is directed to a ferroceneylphosphine ligand of formula (II),

Abstract: The present invention provides an improved process for producing ketorolac tromethamine. The preferred method utilizes a three-part solvent system, comprising isopropanol, ethyl acetate and water.

Abstract: Unsaturated imidosilanes which are essentially free of siloxanes are taught herein for use surface treatments for inorganic solid materials. Novel methods to make such silanes, which do not yield water or siloxanes as a by-product are also taught. Compositions consisting essentially of imidosilane treated inorganic solid materials, resinuous materials and optionally a free radical generator, especially glass fiber reinforced composites, are taught.

Abstract: Processes for the preparation of taxol and other taxanes through selective derivatization of the C(7) and C(10) hydroxyl groups of 10-DAB, particularly a novel process using a new strategy in which the C(10) hydroxyl group is protected or derivatized prior to the C(7) hydroxyl group; and the provision of C(7) and C(10) derivatized 10-DAB compounds.

Abstract: The present invention provides convergent processes for preparing myxopyronins and corallopyronins, compounds useful as antibacterial therapeutics. The present invention also provides novel compositions of matter which are useful for the preparation of pyronin antibiotics.

Abstract: There are disclosed an industrially favorable process for producing a tetrazole compound of general formula (1): characterized in that a nitrile of general formula (2): R1CN  (2) is reacted with hydrazine or a salt thereof in the presence of a catalyst, followed by reaction with a nitrous acid compound of general formula (3): ANO2  (3) or a nitrile of general formula (2) is reacted with hydrogen sulfide, followed by reaction with an alkyl halide of general formula (4): R4J  (4) with hydrazine or a salt thereof, and then with a nitrous acid compound of general formula (3); and an intermediate of general formula (5): R1C(═R5)R6  (5) which is useful for the production of the tetrazole compound (in which R1 to R6, A and J in the above formulas are as defined in the specification).

Abstract: The present invention describes for the first time the design and synthesis of a soluble tumor-directed paclitaxel prodrug which may establish a new mode of utilization of the taxane class of anticancer agents in cancer therapy.

Abstract: A substituted cyclopentene derivative of the formula (VII): wherein R is a hydrogen atom, alkyl radical having 1 to 6 carbon atoms, alkenyl radical having 2 to 6 carbon atoms, alkynyl radical having 2 to 6 carbon atoms, cycloalkyl radical having 3 to 8 carbon atoms, aralkyl radical having 7 to 19 carbon atoms, aryl radical having 6 to 12 carbon atoms, alkoxy radical having 1 to 6 carbon atoms, alkenyloxy radical having 2 to 6 carbon atoms, alkylthio radical having 1 to 6 carbon atoms or alkenylthio radical having 2 to 6 carbon atoms; X1 is (&agr;-OZa, &bgr;-H) or (&agr;-H, &bgr;-OZa), X3 is (&agr;-OZd, &bgr;-H), (&agr;-H, &bgr;-OZd) or oxygen atom, each of Za and Zd, which may be the same or different, is a hydrogen atom or a protective radical for a hydroxyl radical.

Abstract: The invention relates to precursors of the A-ring of vitamin D, of the formula (I): in which A, R, R1 and R2 are as defined in the specification. The invention also relates to a method of preparing compounds (I) comprising the enzymatic asymmetrization of 3,5-dihydroxybenzoic acid derivatives, as well as intermediates of preparation of said compounds.

Abstract: Trans-xanthophyll ester concentrates having a trans-xanthophyll ester content of at least four times greater and preferably at least nine times greater than the cis-xanthophyll ester content are obtained. Xanthophyll ester concentrates having a total xanthophyll ester content of at least 40 wt. % and preferably greater than about 55 wt. % are also obtained.

Abstract: A new process is disclosed, particularly simple, convenient and practical, for the direct synthesis of metallocenes of formula (I): (CP)(ZR1m)n(A)rMLpL′q wherein (ZR1m)n is a divalent group bridging Cp and A; Cp is a substituted or unsubstituted cyclopentadieryl group; A is —O—, —S—, —N(R2)—, wherein R2 is hydrogen, alkyl, cycloalkyl aryl, alkylaryl or arylalkyl, or A has the same meaning of Cp; M is a transition metal belonging to group 3, 4, 5, 6 or to the lanthanide or actinide groups; L is a monoanionic sigma ligand, such as alkyl, cycloalkyl, aryl, alkylaryl or arylalkyl, optionally containing Si or Ge; L′ is halogen or —OR5, R5 being a hydrocarbon radical; m is 1 or 2; n is 0-4; r is 0 or 1; p is 1-3; q is 0-2.

Abstract: The invention relates to stable trimer isopropoxyalane of composition H5Al3(OiPr)4, wherein iPr is a (CH3)2CH radical. The invention also relates to a method for producing stable trimer isopropoxyalane, wherein AlH3 is reacted with Al(OiPr)3 or isopropanol in a molar ratio of 5:4 or 3:4 in a solvent or solvent mixture. The stable trimer isopropoxyalane is particularly suitable for use as a reducing agent in organic and inorganic synthesis, as a source for aluminium or aluminium oxide in the electronics or ceramics industry or to produce pigments.

Abstract: Chlorine-free tetraalkoxysilanes of formula (I) (R1O)4Si  (I) wherein R1 is, independently in each instance, an unbranched, branched, and/or cyclic C1-6 hydrocarbon group is continuously manufactured by a process, comprising: reacting metallic silicon powder with a monohydric alcohol in the presence of a basic catalyst comprising a mixture of: (a) at least one compound of formula (II) [R2O—(R3O)m]nSi)OR1)4-n  (II) (b) at least one compound of formula (III) R2O—(R3O)m—M, and  (III) (c) at least one compound of formula (IV) R2O—(R3O)m—H  (IV) wherein R1 is as defined above; R2 represents, independently in each instance, a C1-10 hydrocarbon group, or hydrogen; R3 represents, independently in each instance, a C1-4 hydrocarbon group; M represents an alkali metal selected from the group consisting of Li, Na, and K; m is zero or a number in the range of 1-20; and n is zero or a number in the range of 1-4; further comprisin

Abstract: A process for the preparation of organosilanes functionalized in the 3-position, by the reaction of suitable allyl compounds with hydrogen silanes, using platinum catalysts having one or more sulfur-containing ligands.

Abstract: A phosphonic acid ester compound of the formula: R1C(SR3)═CHP(═O)(OR2)2 or [P(═O)(OR2)2]CH═C(SR3)—R4—C(SR3)═CH[P(═O)(OR2)2] wherein R1 represents a monovalent group selected from hydrogen, alkyl, cycloalkyl, cycloalkenyl, aryl, aralkyl, alkenyl and silyl, R2 and R3 each represent aryl and R4 represents alkylene or cycloalkylene. The ester compound is produced by reaction of an acetylene compound, R1C≡CH or HC≡C—R4—C≡CH, with with a phosphorothioate, (R2O)2P(═O)SR3, in the presence of a palladium complex catalyst.

Abstract: An improved method for producing an aromatic carbonate by reacting an aromatic hydroxy compound, carbon monoxide and oxygen in the presence of a catalyst system comprising at least one of palladium or a palladium compound; at least one lead compound; at least one halide source; and at least one desiccant, wherein the ratio of equivalents of lead co-catalyst relative to equivalents of palladium catalyst is optimized to increase reaction rate, as well as to allow production of aromatic carbonate in an economically feasible continuous process.

Abstract: Disclosed is a process for the preparation and recovery of cyclopropylacetonitrile by a novel combination of process steps beginning with a mixture of cyclopropylmethyl halide, a cyclobutyl halide and a 4-halo-1-butene. The process permits the recovery of substantially pure cyclopropylacetonitrile and cyclobutyl halide, e.g., cyclopropylacetonitrile and cyclobutyl halide each having a purity greater than about 95%.

Abstract: Use of 4,4-diarylbutadienes of the formula I, where the variables have the meanings explained in the description, as water-soluble photostable UV filters in cosmetic and pharmaceutical preparations for protecting the human skin or human hair from the sun's rays, alone or together with compounds which absorb in the UV region and are known per se for cosmetic and pharmaceutical preparations.

Abstract: An alkyl nitrite can be produced on an industrial scale with a high efficiency and with a low yield of by-products by the process wherein nitrogen oxide-containing feed gas is brought into an alkyl alcohol liquid in a distillation column reactor while circulating a liquid fraction, produced in the reactor and containing the alkyl alcohol, through a circulation path including a lower section of the reactor and a cooler to remove the reaction heat vigorously generated in the reactor, and while controlling the weight ratio of the circulating liquid fraction to the total alkyl alcohol fed into the reactor to 50:1 to 200:1, the molar ratio of the total alkyl alcohol fed to the reactor and contained in the circulating liquid fraction to nitrogen oxide in the feed gas to 20:1 to 150:1, and the content of the alkyl alcohol in the liquid fraction to 15 to 60% by weight; and the resultant gas fraction containing the target alkyl nitrite is collected from the reactor.

Abstract: This invention relates to certain tricyclic compounds that are integrin receptor antagonists.

Abstract: A tetraester of 3,3′,4,4′-biphenyltetracarboxylic acid is advantageously prepared by a process composed of a step of dimerizing an o-phthalic diester in the presence of a catalyst comprising a powdery palladium salt having a specific surface area of at least 0.5 m2/g and a basic bidentate ligand compound and one or more steps of continuing the dimerization after supplemental addition of at least one of the powdery palladium salt and the basic bidentate ligand compound.

Abstract: Disclosed is a process for the preparation of cyclopropylglycine by a 5-step process wherein cyclopropanecarboxaldehyde is reacted with an &agr;-aminoalkylaromatic compound to obtain an imine which is reacted with a cyanide to produce an aminonitrile compound; the aminonitrile compound is hydrolyzed to the corresponding aminocarboxylic acid and finally the arylalkyl residue is removed from the amino group by hydrogenolysis.

Abstract: A process of producing benzoic acids from phthalimides is described. The ability to dramatically reduce the reaction time in comparison to currently practiced processes by the addition of readily available compounds is demonstrated.

Abstract: &agr;-Hydroxycarbonyl compounds are obtained from aldehydes or ketones by forming an acetal or ketal which is decomposed to a vinyl ether. The ether is selectively oxidized under conditions yielding an &agr;-hydroxy-aldehyde or &agr;-hydroxy-ketone with the carbonyl group protected. The last-mentioned compounds are valuable sources for other functional organic molecules, for example lactic acid.

Abstract: The halogenation of a compound of formula (1) or formula (2′), wherein Q is an NH2 group optionally in the form of an addition salt, or an NHCOCH3 group, and X is a halogen atom, using a compound of formula X2, in a solvent selected from an anhydrous halogenated hydrocarbon, a mixture of water and a halogenated hydrocarbon and optionally the compound of formula (1) itself, gives a 2-amino or 2-acetamido trifluoromethylbenzene halogenated in the 5 position of the benzene ring.

Abstract: Disclosed is a process for selectively producing diaminoalkanes which comprises reacting a dihydric alcohol characterized by two to six carbons, preferably 1,3-propanediol, with excess ammonia and sufficient hydrogen to stabilize a nickel or cobalt-containing hydroamination catalyst, at a temperature of at least 150° C. and a pressure of at least 500 psig, until there is substantial formation of the desired diaminoalkane, wherein said catalyst comprises at least one metal selected from the group consisting of nickel and cobalt, or mixtures thereof, optionally in the presence of one or more promoters, but particularly molybdenum oxide.

Abstract: An improved process for decomposing alkyl or aromatic hydroperoxides to form a decomposition reaction mixture containing the corresponding alcohol and ketone. The improvement relates to decomposing the hydroperoxide by contacting the hydroperoxide with a catalytic amount of a heterogeneous catalyst of Nb or Hf hydroxide or oxide. The improvement also relates to decomposing a secondary hydroperoxide by contacting the secondary hydroperoxide with a catalytic amount of a heterogeneous catalyst of Zr or Ti hydroxide or oxide. The catalysts may optionally be supported on SiO2, Al2O3, carbon or TiO2.

Abstract: A process for preparing a bicyclooctanone, in particular 1,5-dialkylbicyclo[3.2.1]octan-8-one, by reacting a bicyclooctanol, in particular dialkylbicyclo[3.2.1]octan-8-ol, with a. a catalyst applied to an active-carbon support and comprising heteropolyoxometallate anions of vanadium, molybdenum and phosphorus, and also a corresponding alkali-metal, alkaline-earth-metal and/or ammonium counter ion, and b. a gaseous, oxygen-containing oxidizing agent.

Abstract: A process for the manufacture of dihydrocitral, a valuable intermediate, through the catalyzed rearrangement of dihydrodehydrolinalool by carrying out the rearrangement in the presence of a molybdenum compound of the general formula MoO2X2 wherein X signifies an acetylacetonate or halide ion, and a dialkyl or diaryl sulphoxide as the catalyst system, in the presence of an organic acid having a pK value in the range of about 4.0 to about 6.5 and in an aprotic organic solvent.

Abstract: A process for obtaining (per) fluoropolyethers substituted at one or at both end groups with a halogen atom selected from bromine or iodine, having the formula: A—CF2—O—(CF2CF2O)p—(CF2O)q—CF2—B  (III) wherein A=B=halogen; or A=halogen and B=COOH or F, and the halogen is I or Br; p and q are integers such as to give a number average molecular weight (MW) in the range 350-5000 and the ratio p/q=0.5-2.0. The process includes treating di- or poly-acylperoxides having an average equivalent weight in the range 350-5000, of formula: T—CF2—O—[(CF2CF2O)p—(CF2O)q—CF2—CO—O—O——CO—CF2—(OCF2)q—(OCF2CF2)p]y—OCF2—COOH  (II) with a halogen selected from iodine or bromine, in a polyhalogenated organic solvent, at temperatures between 20° and 80° C.

Abstract: Most generally, the invention provides a method for making a neutralized polyether polyol, comprising the steps of a) Polymerizing one or more alkylene oxides in the presence of an alkaline catalyst to form a polyalkylene oxide intermediate; and b) Neutralizing the intermediate, after the polymerization step a) is complete, with an organic acid of general formula where R1 is hydrogen, methyl, or ethyl; R2 is methyl or ethyl; and R3 is an alkyl, aryl, or aralkyl group containing one to twelve carbon atoms. The invention also comprises the novel compositions made by the above process.

Abstract: The present invention relates to a process for working up the residual mother liquors from the production of dihydroxydiarylalkanes (bisphenols) discharged from the process once the bisphenol has been separated.

Abstract: Polyalkyl hydroxyaromatics may be prepared from polyalkylenes and hydroxyaromatics in the presence of an acid catalyst and an organic solvent having a boiling point range with an initial boiling point value of below or about the boiling point of the selected hydroxyaromatic reactants and final boiling point of above or equal to about the boiling point of alkylhydroxyaromatic by-product of the reaction. Using this method, accumulation of undesirable alkylhydroxyaromatic by-product/s in a reaction vessel may be minimized, and/or viscosity of polyalkyl hydroxyaromatic product reduced, allowing for increased ease of transfer and transportation.

Abstract: The present invention relates to a process for preparing hydroxylated aromatics by using hydrogen and oxygen and more particularly, to a process for preparing hydroxylated aromatics by using hydrogen and oxygen with a two-component heterogeneous catalyst. One component consists of porous catalyst containing one of Group VIII B transition metals such as Pd, Pt, Au and Cu, and hydrogen transfer organic compounds such as anthraquinone. The other component consists of a catalyst containing a transition metal selected from Ti, V, and Sn with tetrahedral coordination geometry. The main advantages of this new catalytic system are to 1) overcome the drawbacks of liquid phase oxidation using conventional homogeneous catalysts, 2) avoid use of expensive hydrogen peroxide as an oxidant, and 3) improve the selectivity of the reaction.

Abstract: A process for preparing alkali metal alkoxides of alcohols comprising reacting an alkali metal amalgam with an alcohol having at least 3 carbon atoms in the presence of a powder catalyst comprising a transition metal carbide, nitride or carbonitride, to form a reaction mixture, wherein the reaction mixture is subjected to ultrasound during reaction.

Abstract: In a process for finishing neopentyl glycol by cooling, crystallizing and comminuting a neopentyl glycol melt and subsequent packing of the resulting neopentyl glycol particles in storage or transport containers, the melt is cooled at the commencement of cooling for at least 1/10 minutes without use of a coolant or with use of a coolant having a temperature in the range from 50 to 120° C. and the product is packed at a temperature below 30° C.

Abstract: 1,3-Propanediol is prepared in good yield by hydrogenation of methyl 3-hydroxypropionate in the presence of a copper zinc oxide hydrogenation catalyst. The use of the copper zinc oxide hydrogenation catalyst enables greater productivity in an overall process for preparing 1,3-propanediol from ethylene oxide via methyl 3-hydroxypropionate intermediate.

Abstract: Process for the production of 1,4-butanediol by mixed phase catalytic hydrogenation of gamma-butyrolactone, succinic anhydride esters, or mixtures thereof.

Abstract: A process for the reduction of ketones or aldehydes to alcohols has been developed. The process involves contacting the ketone or aldehyde with a primary or secondary alcohol and a catalyst at reduction conditions. The catalyst is a molecular sieve having the empirical formula: (MwSnxTiySi1-x-y-zGez)O2 where M is a trivalent metal such as aluminum or boron. These molecular sieves have a microporous three dimensional framework structure of at least SiO2 and SnO2 tetrahedral units, a crystallographically regular pore system and the characteristic x-ray diffraction pattern of zeolite beta.

Abstract: This invention relates in part to processes for producing one or more substituted or unsubstituted unsaturated alcohols which comprise reacting one or more substituted or unsubstituted alkadienes with carbon monoxide and hydrogen in the presence of a metal-ligand complex catalyst and a promoter and optionally free ligand to produce said one or more substituted or unsubstituted unsaturated alcohols. The substituted and unsubstituted unsaturated alcohols produced by the processes of this invention can undergo further reaction(s) to afford desired derivatives thereof. This invention also relates in part to reaction mixtures containing one or more substituted or unsubstituted unsaturated alcohols as principal product(s) of reaction.

Abstract: Dinitro aromatic compounds are improvedly prepared by reacting an aromatic compound with a nitric acid nitrating agent and thence separating the nitrating acid from the process stream thus formed, the process stream containing said at least one dinitro aromatic compound and also having a fraction of the nitrating acid dissolved therein, the subject process also comprising (a) distilling/stripping nitric acid from said process stream, (b) recovering nitric acid from the top of the distillation/stripping vessel and recycling same to the nitration reaction and (c) washing the process stream which contains the at least one dinitro aromatic compound, but having the nitric acid removed therefrom.

Abstract: This invention provides a process for preparing 1,1,1,2,3,3,3-heptafluoropropane, which comprises reacting 2-trifluoromethyl-3,3,3-trifluoropropionic acid with fluorine gas. The process according to this invention produces 1,1,1,2,3,3,3-heptafluoropropane with high selectivity and is an industrially efficient and economical method.