Abstract: A process for preparing N-[(1R)-1-(1-naphthyl)ethyl]-3-[3-(trifluoromethyl)-phenyl]propan-1-amine hydrochloride salt of formula (I) i.e. Cinacalcet hydrochloride and its intermediates of formulae (VII) and (VIII) wherein Z is chloride or another pharmaceutically acceptable anionic counterion.

Abstract: The present invention refers to a new process for the synthesis of tapentadol comprising the quantitative resolution of the racemic mixture (V) to obtain the stereoisomer of (S)-3-(dimethylamino)-2-methyl-1-(3-nitrophenyl)-propan-1-one (VII) according to the Scheme 2 below using the (2R,3R)—O,O?-dibenzoyltartaric chiral acid wherein said resolution is quantitative. The present invention also refers to some intermediate compounds of the new synthesis process of tapentadol.

Abstract: Novel materials are provided, having a single phenyl or a chain of phenyls where there is a nitrogen atom on each end of the single phenyl or chain of phenyls. The nitrogen atom may be further substituted with particular thiophene, benzothiophene, and triphenylene groups. Organic light-emitting devices are also provided, where the novel materials are used as a hole transport material in the device. Combinations of the hole transport material with specific host materials are also provided.

Abstract: A process for preparing N-[(1R)-1-(1-naphthyl)ethyl]-3-[3-(trifluoromethyl)-phenyl]propan-1-amine of formula (I) i.e. Cinacalcet and its intermediates of formulae (V), (Va) and (Vb).

Abstract: A process for the preparation of an 1,1-disubstituted oxirane is disclosed, wherein an organic sulphide is reacted in a polar solvent with an educt containing a leaving group attached to a primary or secondary carbon atom, and/or the sulfonium salt formed in this way is reacted with a ketone in presence of a base and a polar solvent. Oxiranes of the type obtained may be further converted into the corresponding ?-hydroxyketone or ?-aminoketone, either in one step by subjecting to aerobic oxidation in the presence of a transition metal catalyst, or in two steps by hydrolyzation in the presence of an aqueous acid to the corresponding dialcohol and subsequent selective oxidation. Further described are some novel epoxide intermediates. The ?-hydroxyketones and ?-aminoketones thus obtainable are useful inter alia as photoinitiators.

Abstract: The present invention discloses both amine compositions and amine-epoxy compositions containing N,N?-dimethyl-meta-xylylenediamine. A novel process for producing amines such as N,N?-dimethyl-meta-xylylenediamine, and structurally similar amines, is also disclosed.

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 an amorphous bupropion hydrobromide and an amorphous bupropion hydrobromide granulates with at least one pharmaceutically acceptable carrier, and a process for its preparation.

Abstract: A process for preparing N-[(1R)-1-(1-naphthyl)ethyl]-3-[3-(trifluoromethyl)-phenyl]propan-1-amine of formula (I) i.e. Cinacalcet and its intermediates of formulae (V), (Va) and (Vb).

Abstract: A process is disclosed for the preparation of a compound of formula and/or an addition salt of a proton acid, wherein R1 and R2 independently represent alkyl, cycloalkyl, aryl or aralkyl, each aryl or aralkyl being optionally further substituted with alkyl, alkoxy and/or halogen. The process involves reacting a mixture comprising a methyl ketone of formula and a compound of formula H2N—R2 (V) and/or an addition salt of proton acid, and formaldehyde in the presence of a solvent selected from the group consisting of water, aliphatic alcohols, cycloaliphatic alcohols and mixtures thereof, and optionally a proton acid to afford a ?-amino ketone of formula and/or an addition salt of a proton acid, and reducing the carbonyl group of said ?-amino ketone to afford a compound of formula I, and/or an addition salt of a proton acid wherein the first step is carried out at a pressure above 1.5 bar.

Abstract: This invention described a synthesis method of bupropion hydrochloride. m-chloropropiophenone was brominated directly with bromine, then aminated with t-butylamine and finally reacted with HCl to obtain crude product of bupropion hydrochloride. Pure product was obtained after recrystallization. This method is convenient and suitable for commercial manufacturing because of low cost of production, high yield, less byproducts and being environmental friendly.

Abstract: A benzylamine derivative has a structure represented by the following formula (1): In a method for optical resolution of the benzylamine derivative, optically active mandelic acid is used as an optical resolving agent. In an optical resolution step in a production method of the optically active benzylamine derivative, an optically active (S)-benzylamine derivative represented by the formula (3) is precipitated as (S)-mandelic acid salt from a solution containing the benzylamine derivative and (S)-mandelic acid: wherein Ar represents an aryl group that has 6 to 15 carbon atoms and may have a substituent, and *1 represents an asymmetric carbon atom.

Abstract: This invention described a synthesis method of bupropion hydrochloride. m-chloropropiophenone was brominated directly with bromine, then aminated with t-butylamine and finally reacted with HCl to obtain crude product of bupropion hydrochloride. Pure product was obtained after recrystallization. This method is convenient and suitable for commercial manufacturing because of low cost of production, high yield, less byproducts and being environmental friendly.

Abstract: Non-steroidal androgen receptor modulating compounds of the general formula (I), their pharmaceutically acceptable salts, preparation process and pharmaceutically compositions containing the said compounds are disclosed. Such compounds of the general formula (I) or their pharmaceutically acceptable salts can be used for preparing non-steroidal medicines to treat and/or prevent conditions or diseases such as prostatic hyperplasia, prostate cancer, hirsutism, severe hormone-dependent alopecia or acne, etc. as a result of androgen receptor antagonistic activities.

Abstract: Compounds of formula (I) where: {R1 is methyl, ethyl, cycloalkyl or optionally substituted aryl; Z is arylene or a group of formula —(CHR4)n-, where R4 is hydrogen, hydroxy or alkyl, and n is a number from 0 to 6; Y is carbonyl or a —CH2— group; Q is a residue of a mono- or poly-hydroxyl compound having from I to 6 hydroxy groups; and x is a number from I to 6; and esters thereof} are useful as sensitizers for use in radiationcurable compositions.

Abstract: Provided is a process for preparing Cinacalcet, (R)-?-methyl-N-[3-[3-(trifluoromethyl)phenyl]propyl]-1-naphthalenemethane amine and intermediates thereof.

Abstract: A process for easily producing an optically active ?-amino alcohol useful as a pharmaceutical intermediate from an inexpensive, readily available starting material is provided. A readily available ?-substituted ketone is reacted with an optically active amine to yield a diastereomer mixture of an optically active ?-substituted aminoketone. One of the diastereomers is isolated optionally after the diastereomers are converted to salts with an acid. The optically active ?-substituted aminoketone or a salt thereof thus isolated was stereoselectively reduced to yield an optically active ?-substituted amino alcohol. The optically active ?-substituted amino alcohol is subjected to hydrogenolysis to produce an optically active ?-amino alcohol or a salt thereof.

Abstract: The present invention concerns a method of synthesizing fluoxetine hydrochloride. The method includes the synthesis of 3-methylamino-1-phenyl-1-propanol by reduction of 1-phenyl-3-methylamino-2-propen-1-one with sodium borohydride and acetic acid.

Abstract: The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I 1

Abstract: The present invention concerns a method of synthesizing fluoxetine hydrochloride. The method includes the synthesis of 3-methylamino-1-phenyl-1-propanol by reduction of 1-phenyl-3-methylamino-1-propen-1-one with sodium borohydride and acetic acid.

Abstract: An amino group of an &agr;-amino acid ester is protected as an imine, and it is then reacted with a halomethyllithium to obtain an N-protected-&agr;-aminohalomethylketone. Further, this N-protected-&agr;-aminohalomethylketone is treated with an acid to obtain an &agr;-aminohalomethylketone. This process is suited for industrial production, and can produce an &agr;-aminohalomethylketone and its related compounds economically and efficiently.

Abstract: The present invention provides a commercially profitable process for producing a &bgr;-amino acid ester derivative

Abstract: An amino group of an &agr;-amino acid ester is protected as an imine, and it is then reacted with a halomethyllithium to obtain an N-protected-&agr;-aminohalomethylketone. Further, this N-protected-&agr;-aminohalomethylketone is treated with an acid to obtain an &agr;-aminohalomethylketone. This process is suited for industrial production, and can produce an &agr;-aminohalomethylketone and its related compounds economically and efficiently.

Abstract: Herein is disclosed a process for producing an &agr;-aminohalomethyl ketone derivative which comprises subjecting to catalytic reduction the corresponding &agr;-aminodihalomethyl ketone derivative, and which process is efficient and suited for industrial production thereof.

Abstract: Novel, stable formulations of bupropion hydrochloride are provided which will maintain at least 80% of initial bupropion hydrochloride potency after one year. Methods of inhibiting degradation of bupropion hydrochloride and methods of preparing stable formulations of bupropion hydrochloride are also provided.

Abstract: An inclusion complex of bupropion hydrochloride with beta cyclodextrin that stabilizes the bupropion hydrochloride against degradation. A method of preparing an inclusion complex of bupropion hydrochloride with beta cyclodextrin that stabilizes the bupropion hydrochloride against degradation. A novel stabilized sustained-release pharmaceutical composition of bupropion hydrochloride containing an inclusion complex of bupropion hydrochloride with beta cyclodextrin. A method of preparing a novel stabilized sustained-release pharmaceutical composition containing an inclusion complex of bupropion hydrochloride with beta cyclodextrin.

Abstract: Disclosed are methods of producing of alkoxy arylamine compounds which find particular use in the syntheses of pharmaceutical drug. The alkoxy arylamine compounds generally have the formula: H2N—Ar—OR wherein Ar is an unsubstituted or substituted aromatic group, and R is an unsubstituted or substituted alkyl or aryl group. The methods comprise generally, the steps of (a) alkylating a protected-amino arylalcohol to form a protected-amino arylether; and (b) deprotecting said protected-amino arylether to form an alkoxy arylamine compound.

Abstract: Mannich polyols having a viscosity of from 300 to 3,500 cps (0.3 to 3.5 Pa*s) at 25° C. are prepared by admixing a phenol, an alkanolamines, and formaldehyde mixed in molar ratios of from 1:1:1 to 1:2.2:2.2 resulting in an initiator which can be alkoxylated using a mixture of ethylene oxide and propylene oxide to prepare polyols that have a nominal functionality of from 3 to 5.4.

Abstract: A novel process for the preparation of compounds of formula I by aminolysis of a p-halophenyl alkyl ketone of formula II with a cyclic amine of formula III in water at a temperature of at least 130° C., in which formulae X is a halogen atom and R1, R2 and R3 are as claimed in claim 1, as well as the novel compounds of formula I and their use for the preparation of photoinitiators for the photopolymerisation of ethylenically unsaturated compounds.

Abstract: N-protected/N-substituted alpha-amino aldehydes, which are useful as pharmaceuticals and pharmaceutical intermediates, can be stored and shipped in a more stable form as N-protected/N-substituted-beta-amino hydroxy sulfonates which can be readily converted back into the aldehyde under mild conditions. The present invention relates to N-protected/N-substituted-beta-amino hydroxy sulfonates and their preparation and use.

Abstract: This invention provides a process for preparing acylaromatics comprising reacting an aromatic compound with a carboxylic acid in the presence of a reaction medium comprising polyphosphoric acid and a strong protic acid. In one embodiment, the invention provides a process for preparing a para-acyl phenoxyethylamine comprising the steps of reacting a 2-phenoxyethyl compound bearing a leaving group on the ethyl 1-position with a carboxylic acid in the presence of a reaction medium comprising polyphosphoric acid and a strong protic acid, to form apara-acyl phenoxyethyl intermediate bearing the leaving group; and reacting the para-acyl phenoxyethyl intermediate with an amine that substitutes for the leaving group to form the para-acyl phenoxyethylamine.

Abstract: N-protected/N-substituted alpha-amino aldehydes, which are useful as pharmaceuticals and pharmaceutical intermediates, can be stored and shipped in a more stable form as N-protected/N-substituted-beta-amino hydroxy sulfonates which can be readily converted back into the aldehyde under mild conditions. The present invention relates to N-protected/N-substituted-beta-amino hydroxy sulfonates and their preparation and use.

Abstract: The present invention discloses a process for the preparation of a compound having formula 4: ##STR1## The process comprises the step of reacting an enolate having the formula: ##STR2## with a Grignard reagent. The enolate salt is formed in situ from the reaction of a protected ester wherein M is an alkali metal. R.sub.6 and R.sub.7 are each hydrogen or are independently selected from ##STR3## wherein R.sub.a and R.sub.b are independently selected from hydrogen, lower alkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, lower alkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR4## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from lower alkyl, trifluoromethyl, alkoxy and halo. Alternatively, R.sub.6 is as defined above and R.sub.7 is R.sub.12 OC(O)-- wherein R.sub.12 is benzyl; or R.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded form ##STR5## wherein R.sub.

Abstract: A novel process for the preparation of compounds of formula I ##STR1## by aminolysis of a p-halophenyl alkyl ketone of formula II ##STR2## with a cyclic amine of formula III ##STR3## in water at a temperature of at least 130.degree. C., in which formulae X is a halogen atom and R.sub.1, R.sub.2 and R.sub.3 are as claimed in claim 1, as well as the novel compounds of formula I and their use for the preparation of photoinitiators for the photopolymerisation of ethylenically unsaturated compounds.

Abstract: A process for producing a (4S)-4-(N,N-dibenzyl)amino-5-phenyl-3-oxo-pentanenitrile derivative which comprises reacting a (2S)-2-(N,N-dibenzyl)aminophenylalanine ester derivative with acetonitrile in the presence of a lithium compound or a magnesium compound is disclosed, and a process for producing a (2S)-2-(N,N-dibenzyl)amino-5-amino-1,6-diphenyl-4-hexen-3-one derivative which comprises adding a benzylmagnesium halide or a benzyllithium to a reaction solution containing the (4S)-4-(N,N-dibenzyl)amino-5-phenyl-3-oxo-pentanenitrile derivative and reacting the derivative with the benzylmagnesium halide or the benzyllithium is also disclosed. According to these processes, optically pure (4S)-4-(N,N-dibenzyl)amino-5-phenyl-3-oxo-pentanenitrile derivative and (2S)-2-(N,N-dibenzyl)amino-5-amino-1,6-diphenyl-4-hexen-3-one derivative can be produced in a good yield on an industrial scale.

Abstract: The present invention relates to a method of forming a 1,3-diamino-3-substituted-2-propanol chemical intermediate from which various chemicals, such as selected protease-inhibitors and other drugs, as well as polymers, can be synthesized.This method includes contacting a nitromethyl amino acid compound with at least one reducing agent to form the 1,3-diamino-3-substituted-2-propanol chemical intermediate.

Abstract: The present invention relates to a method of forming a 1,3-diamino-3-substituted-2-propanol chemical intermediate from which various chemicals, such as selected protease-inhibitors and other drugs, as well as polymers, can be synthesized.This method includes contacting a nitromethyl amino acid compound with at least one reducing agent to form the 1,3-diamino-3-substituted-2-propanol chemical intermediate.

Abstract: The present invention relates to a method of forming a 1,3-diamino-3-substituted-2-propanol chemical intermediate from which various chemicals, such as selected protease-inhibitors and other drugs, as well as polymers, can be synthesized.The method includes contacting a nitromethyl amino acid compound with at least one reducing agent to form the 1,3-diamino-3-substituted-2-propanol chemical intermediate.

Abstract: This invention comprises polyanionic benzylglycosides of benzene triacid amides of the general formula I ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are, independently, H, SO.sub.3 M, or ##STR2## and each oligosaccharide group contains 1 to 3 sugar groups; M is lithium, sodium, potassium, or ammonium;n is 1 or 2;X is a halogen, lower alkyl having 1 to 6 carbon atoms, or lower alkoxy having 1 to 6 carbon atoms;Y is carbonyl or sulfonyl;or the pharmaceutically acceptable salts thereof, as well as their use as smooth muscle cell antiproliferation inhibitors and as therapeutic compositions for treating diseases and conditions which are characterized by excessive smooth muscle proliferation.

Abstract: The invention relates to new N,N,N'N'-tetra-substituted-1,2-ethanediamine compounds of the general formula (I): ##STR1## wherein X is a carbonyl (CO), hydroxymethylen (CHOH) or p-fluorophenyl-methylen (p--F--C.sub.6 H.sub.4 --CH) group and R is a benzyl group optionally substituted in p-- with an halogen, or R is a 2-pyrimidinyl group with the proviso that simultaneously X may not be p-fluorophenyl-methylen (p--F--C.sub.6 H.sub.4 --CH) and R may not be an unsubstituted benzyl group, as well as their pharmaceutically acceptable additions salts.The compounds are potentially useful in the treatment of sigma receptor-related nervous system diseases.

Abstract: A process for the selective oxidation of a primary or secondary alcohol to an aldehyde or ketone and for the oxidation of a 1,2-diol to an .alpha.-ketol or .alpha.-diketone, which comprises contacting the alcohol or 1,2-diol with o-iodoxybenzoic acid. This process is suited for selective oxidation of alcohols containing easily oxidizable groups, such as amino or thioether groups and easily oxidizable heterocycles.

Abstract: The present invention relates to a method of forming a 1,3-diamino-3-substituted-2-propanol chemical intermediate from which various chemicals, such as selected protease-inhibitors and other drugs, as well as polymers, can be synthesized.This method includes contacting a nitromethyl amino acid compound with at least one reducing agent to form the 1,3-diamino-3-substituted-2-propanol chemical intermediate.

Abstract: Arylketoamines are prepared by reacting arylisonitrosoalkanones with hydrogen in the presence of a transition metal catalyst and a liquid carboxylic acid at a temperature of less than about 600.degree. C.

Abstract: Arylketoamines are prepared by reacting arylisonitrosoalkanones with hydrogen in the presence of a transition metal catalyst and a liquid carboxylic acid at a temperature of less than about 60.degree. C.

Abstract: A catalytic asymmetric reduction process, which, by hydrogenating trisubstituted olefins, yields a corresponding organic compound having a high level of enantiomeric purity is disclosed. The reduction process utilizes a chiral metal catalyst that includes a metal or metal complex that is selected from groups 3, 4, 5, or 6, lanthanides and actinides. Moreover, the process uses hydrogen as the stoichiometric reducing agent and may be carried out at pressures ranging from about 1 to 200 atmospheres.

Abstract: A new process for the preparation of pyrazolines of formula ##STR1## is provided, in which R.sup.1 and R.sup.3 are identical or different and each represent optionally substituted aryl or optionally substituted and/or benzo-fused heterocyclyl with 5 or 6 ring members of which 1 to 4 are nitrogen atoms and the remainder are carbon atoms, andR.sup.2 represents hydrogen or alkyl, cycloalkyl or aryl, each of which is optionally substituted.In this, in a first reaction stage, ketones of formula (II) ##STR2## are reacted with bis-dialkylaminomethanes of formula (III)(R.sup.4).sub.2 N--CH.sub.2 --N(R.sup.4).sub.2 (III)in whichR.sup.4 represents alkyl,optionally in the presence of a diluent, at temperatures between 0.degree. C. and 100.degree. C. and the substituted dialkylaminoalkyl ketones of general formula (IV) ##STR3## formed in this way are optionally isolated and in a second process stage are reacted with hydrazine (hydrate), optionally in the presence of a diluent, at temperatures between 0.degree. C.

Abstract: Arylketoamines are prepared by reacting arylisonitrosoalkanones with hydrogen in the presence of a transition metal catalyst and a liquid carboxylic acid at a temperature of less than about 60.degree. C.

Abstract: A process for preparing an optically active 2-aminopropanal through oxidative cleavage of the corresponding optically active 3-amino-1,2-butanediol of the following formula (2): ##STR1## wherein R1 is a hydrocarbon group having 3 to 6 carbon atoms; R2 and R3 are each a hydrogen atom, or separately or together represent an N-protecting group; and the configuration at the *1 position is S or R. An optically active 2-aminopropanal of high purity can be obtained in a high yield by the process.

Abstract: A process for making unsaturated .alpha.-amines from olefins wherein the process includes adding an aminating agent, an olefin and a molybdenum based catalyst to a reaction vessel having a nitrogen atmosphere. The catalyst may be described by the general formula LL'MoO.sub.2, L.sub.2 L'MoO.sub.2, or LL'MoO(X--Y).

Abstract: A process for preparing p-nitroaromatic amides is provided which comprises contacting a nitrile, nitrobenzene, a suitable base and water in the presence of a suitable solvent system to form a mixture, and reacting the mixture at a suitable temperature in a confined reaction zone in the presence of a controlled amount of protic material. The p-nitroaromatic amides of the invention can be reduced to p-aminoaromatic amides. In one embodiment, the p-aminoaromatic amide is further reacted with ammonia under conditions which produce the corresponding p-aminoaromatic amine and the amide corresponding to the nitrile starting material or with water in the presence of a suitable basic or acidic catalyst under conditions which produce the corresponding p-aminoaromatic amine and the acid or salt thereof corresponding to the nitrile starting material. In another embodiment, the p-aminoaromatic amine is reductively alkylated to produce alkylated p-aminoaromatic amine.