Abstract: The (S,S) optical isomer of a compound having the general formula ##STR1## wherein R and R.sub.1-5 are as defined herein, is recovered essentially free of the (R,S) and (S,R) isomers, by forming a solution of the esters of the (S,S) and the (R,S) and/or (S,R) isomers of said compound, selectively precipitating an acid salt (e.g. maleate) of the (S,S) ester from the solution, and treating the precipitate to form the desired free acid.

Abstract: The present invention relates to a process for preparing optically active phenylalanine which comprises resolving mixture of a complex of D-phenylalanine and optically active mandelic acid and a complex of L-phenylalanine and optically active mandelic acid in a solvent containing hydrochloric acid, carboxylic acid, phosphoric acid or a salt thereof to obtain the complex having lower solubility, and removing said optically active mandelic acid from the obtained complex to obtain an optically active phenylalanine.In the case of resolving DL-phenylalanine by the process according to the present invention, the amount of mother liquor used in resolution can be made to about 1/2 to 1/6 as compared to the amount of mother liquor of which the acidic compound or the salt thereof is not used in the resolution. Accordingly, the process according to the present invention is extremely profitable as an industrial process for producing an optically active phenylalanine.

Abstract: This invention relates to a process for the preparation of free L .alpha.-amino acids by the complete conversion of their D antipodes taken individually or possibly in racemic mixtures.The process according to the present invention is characterized in that the D antipodes of an ester of said .alpha.-amino acid is racemized in the presence of a chemical catalyst formed by at least one aromatic aldehyde corresponding to the general formula: ##STR1## wherein: Ar represents an aromatic ring optionally containing a heteroatom, such as nitrogen, andB represents a basic function,to produce a mixture in dynamic equilibrium of the two forms D and L of said ester, the ester which is present in the L form is hydrolyzed enzymatically and irreversibly to produce the corresponding stereostable L .alpha.-amino acid, said stages of chemical racemization and of enzymatic hydrolysis being carried out under identical reaction conditions, and the free L .alpha.-amino acid is recovered.

Abstract: A method for the extraction of certain amino acids from aqueous solutions by contacting said solutions with various dithiophosphinates in conjunction with a polar diluent is disclosed.

Abstract: Intermediates of the formula ##STR1## are disclosed. These compounds are useful in preparing substituted peptide compounds which possess hypotensive and analgesic activity.

Abstract: N-substituted amino acids are described which when coupled with 1,2,3,4-tetrahydroisoquinolines result in substituted acyl derivatives of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids as anti-hypertensive agents. The novel intermediates are in turn prepared by reacting an amino acid such as alanine with 2-bromo-4-phenyl butanoic acid or an ester thereof.

Abstract: An aminocarboxylic acid derivative represented by the formula ##STR1## wherein R.sub.1 and R.sub.2, independently from each other, represent a hydrogen atom or an alkyl group which may have a substituent, and Y represents --NH-- or --S--, provided that when Y represents --NH--, at least one of R.sub.1 and R.sub.2 represents an alkyl group which may have a substituent. These compounds have excellent inhibitory activity on dipeptidase in animals, and are useful for administration in combination with carbapenem antibiotics.

Abstract: The present invention relates to the preparation of mixtures of sterically hindered substituted N-secondary amino acids or their alkali metal salts by a one-step reductive condensation of an amino acid or its alkali metal salt containing a primary amino group and a ketone to thereby form a mono-substituted amino acid or alkali metal salt thereof, followed by preparing the corresponding sterically hindered tertiary amino acids or alkali metal salt thereof by reacting the mono-substituted amino acids or alkali metal salt thereof with an unhindered aldehyde under reducing conditions in the presence of a hydrogenating catalyst. The novel mixtures of the sterically hindered mono-substituted amino acids and the tertiary amino acids and their alkali metal salts are useful promoters for alkaline salts in "hot pot" acid gas scrubbing processes.

Abstract: .alpha.-(S)-amino acid..alpha.-phenylethanesulfonate compounds and methods of optical resolution of .alpha.-amino acids and .alpha.-phenylethanesulfonic acids are described.

Abstract: A process for preparing .alpha.-alkyl amino acids by enantioretentive .alpha.-alkylation of .alpha.-amino acids is described. The products are bioactive compounds including some useful as therapeutic agents.

Abstract: Amino acid fractions of different composition are obtained at different times by fractional filtration after neutralization of the hydrolysates. Tyrosine-rich and leucine-rich fractions are specifically treated and lead to the recovery of L-tyrosine, L-cystine, L-leucine and L-phenyl-alanine.

Abstract: The invention relates to crystallized 2-dimethylamino-2-parahydroxyphenyl sodium acetate, anhydrous or with 2 molecules of water. The process for preparation thereof comprises heating parahydroxy mandelic acid in dimethylformamide in the presence of a catalytic quantity of a strong acid, such reaction being followed by a sodium hydroxide neutralization. Said product is applied to the production of parahydroxybenzyl cyanide by reacting it with 2-hydroxy isobutyronitrile.

Abstract: A process for producing efficiently and economically without using strong acids nor strong bases, .alpha.-amino acids from .alpha.-amino acid amides by hydrolyzing .alpha.-amino acid amides in an aqueous medium in the presence of ammonia. If necessary, the resultant hydrolyzate liquid from which .alpha.-amino acid has been removed may be reused.

Abstract: Provided is a method of increasing the purity of amphoteric compound compositions. The method is: (a) providing an amount of a crude amphoteric compound composition, (b) using a portion of the crude composition to prepare in solution a cationic salt of the amphoteric compound, (c) using another portion of the crude composition to prepare in solution an anionic salt of the amphoteric compound, (d) mixing together the solutions wherein a precipitate is formed, and (e) collecting the precipitate which is an amphoteric compound composition of higher purity than the crude composition.

Abstract: Aqueous solutions of sodium salts of .alpha.-aminocarboxylic acids practically free of foreign salts are produced by saponifying the corresponding hydantoin at a temperature between 110.degree. C. and 180.degree. C. with a mixture, in each case based on the hydantoin, of 1 equivalent of sodium hydroxide and 2 equivalents of calcium oxide or hydroxide, separating off the precipitated calcium carbonate after the end of the saponification and concentrating the aqueous sodium salt solution remaining to drive off the ammonia contained therein.

Abstract: A compound represented by the following formula ##STR1## wherein R.sup.1 represents a hydrogen atom, an acyl group or an alkoxycarbonyl group; X.sup.1 represents an alkylene group having 3 to 6 carbon atoms, a 1,4-cyclohexylene group, or a 1,4-phenylene group, the alkylene group may be substituted by an alkyl group having 1 to 6 carbon atoms, and the 1,4-phenylene group may be substituted by 1 or 2 substituents selected from halogen atoms and alkoxy groups having 1 to 6 carbon atoms; R.sup.2 represents a hydrogen atom or a hydroxyl group and R.sup.3 represents hydrogen atom, or R.sup.2 and R.sup.3 together may form an oxo group (.dbd.O), and when X.sup.1 is other than the 1,4-phenylene group, R.sup.2 represents a hydrogen atom and R.sup.3 represents a bond between the carbon atoms to which R.sup.3 is bonded and that carbon atom of X.sup.1 which is adjacent to said carbon atom; X.sup.

Abstract: A process for preparing an alkali salt of d,l-phenylalanine and the free acid thereof is disclosed. According to the invention an alkali salt of phenylpyruvic acid is reacted at elevated pressure with hydrogen and ammonia in the presence of a noble metal catalyst of Group VIII. If the acid is desired it is obtained by acidification of the corresponding salt.

Abstract: New quinone derivatives of the formula: ##STR1## wherein R.sup.1 is methyl or methoxy, or two of R.sup.1 combine to represent --CH.dbd.CH--CH.dbd.CH--, R is amino which may be substituted or --OR.sup.4 wherein R.sup.4 is hydrogen, C.sub.1-4 alkyl or --CH.sub.2 --CH.dbd.C(CH.sub.3 --CH.sub.2 --.sub.m H (wherein m is an integer of 1 to 10), and n is an integer of 1 to 10 when R is amino which may be substituted, or n is an integer of 2 to 10 when R is --OR.sup.4, and their hydroquinone forms, have useful physiological activities such as blood-pressure decreasing and antiallergic activities.

Abstract: The present invention refers to N-Benzoyl-.omega.

Abstract: A method for synthesizing alpha amino acids proceeding through novel intermediates of the formulas:R.sub.1 R.sub.2 C(OSOCl)CN, R.sub.1 R.sub.2 C(Cl)CN and [R.sub.1 R.sub.2 C(CN)O].sub.2 SOwherein R.sub.1 and R.sub.2 are each selected from hydrogen monovalent substituted and unsubstituted hydrocarbon radicals of 1 to 12 carbon atoms. The use of these intermediates allows the synthesis steps to be exothermic and results in an overall synthesis method which is faster than the synthesis methods of the prior art.

Abstract: Compounds of the formula ##STR1## wherein X is an imino acid or ester and R.sub.1 is hydrogen, ##STR2## are useful hypotensive agents due to their angiotensin converting enzyme inhibition activity.

Abstract: Alkali metal aminoalkanoate is prepared by contacting in the presence of an alkali metal carboxylate a reaction mixture in which there is at least one alkali metal hydroxide, at least one lactam, and water. Arylene sulfide polymer is prepared by contacting at polymerization conditions a reaction mixture that contains at least one alkali metal aminoalkanoate prepared as described above; at least one polyhalo-substituted aromatic compound; at least one organic amide as solvent and H.sub.2 S. In an embodiment of the polymerization the organic amide used as solvent can be the same as the lactam from which the alkali metal aminoalkanoate was produced.

Abstract: A method for synthesizing alpha amino acids proceding through novel intermediates of the formulas: R.sub.1 R.sub.2 C(OSOCl)CN, R.sub.1 R.sub.2 C(Cl)CN and [R.sub.1 R.sub.2 C(CN)O].sub.2 SO wherein R.sub.1 and R.sub.2 are each selected from hydrogen monovalent substituted and unsubstituted hydrocarbon radicals of 1 to 12 carbon atoms. The use of these intermediates allows the synthesis steps to be exothermic and results in an overall synthesis method which is faster than the synthesis methods of the prior art.

Abstract: A method for synthesizing alpha amino acids proceding through novel intermediates of the formulas:R.sub.1 R.sub.2 C(OSOCl)CN, R.sub.1 R.sub.2 C(Cl)CN and [R.sub.1 R.sub.2 C(CN)O].sub.2 SOwherein R.sub.1 and R.sub.2 are each selected from hydrogen monovalent substituted and unsubstituted hydrocarbon radicals of 1 to 10 carbon atoms. The use of these intermediates allows the synthesis steps to be exothermic and results in an overall synthesis method which is faster than the snythesis methods of the prior art.

Abstract: There is described an improved process for the separation and recovery of L-phenylalanine and L-aspartic acid from sidestreams resulting from the preparation of .alpha.-L-aspartyl-L-phenylalanine methyl ester. It has been found that superior separation is obtained by combining one or more of the mother liquor and wash solutions formed during the preparation of .alpha.-L-aspartyl-L-phenylalanine methyl ester, hydrolyzing same to afford the hydrohalide salts of L-aspartic acid and L-phenylalanine, acidifying the hydrolysis solution to precipitate the hydrohalide salt of L-phenylalanine, separating the hydrohalide salt of L-phenylalanine, dissolving it in water and adjusting the pH of the solution to the isoelectric point of L-phenylalanine, thus affording pure L-phenylalanine, and thereafter adjusting the pH of the solution after separation of the L-phenylalanine hydrohalide to the isoelectric point of L-aspartic acid to precipitate L-aspartic acid.

Abstract: Manufacture of 4-substituted oxazolinone-(5) compounds, which are intermediates for substituted aminoacids, by alkylation of 2-substituted or 3,4-disubstituted oxazolinone-(5) compounds in an aprotic solvent in the presence of a tertiary amine.

Abstract: 1-Ethyl-1,4-dihydro-6-(2-naphthyl)-4-oxonicotinic acid and C.sub.1-6 -alkyl esters thereof as well as their alkali metal, alkaline earth metal or ammonium salts are described. The foregoing compounds are useful as central nervous system stimulants. Also described are 1-ethyl-6-(2-naphthyl)-4-oxo-1,4,5,6-tetrahydronicotinic acid and C.sub.1-6 -alkyl esters thereof, which are useful as intermediates.

Abstract: This invention relates to new ammonium salts of .alpha.-ketocarboxylic acids, to their use for the production of amines in situ by photochemical decomposition and to photochemically hardenable coating compositions containing these ammonium salts.

Abstract: Biphenylylalkylamines which have anti-arrhythmic activity have been prepared. Pharmaceutical formulations containing such compounds and a method of treating cardiac arrhythmias are provided.

Abstract: Manufacture of 4-substituted oxazolinone-(5) compounds, which are intermediates for .alpha.-substituted aminoacids, by alkylation of 2-substituted or 3,4-disubstituted oxozolinone-(5) compounds in an aprotic solvent in the presence of a tertiary amine.

Abstract: Process for the homogeneous catalytic hydrogenation of .beta.-substituted-.alpha.-acylamido-acrylic acids which yields, after hydrogenation, an optically active mixture. The process comprises the hydrogenation of .beta.-substituted-.alpha.-acylamidoacrylic acids in the presence of an optically active coordinated metal complex hydrogenation catalyst, in which the metal is selected from the group consisting of rhodium, iridium, ruthenium, osmium, palladium and platinum.This process is a generalized process for any asymmetric hydrogenation of .beta.-substituted-.alpha.-acylamido-acrylic acids in which one .alpha.-amino acid enantiomorph is the desired end-product. It is especially useful for the preparation of .alpha.-amino acids found in nature which possess optical activity and which have a hydrogen attached to the asymmetric center.This invention also relates to new optically active coordinated metal complex hydrogenation catalysts.

Abstract: Novel acetylenic derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein R is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR2## is hydrogen, a straight or branched lower alkyl group of 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; each R.sub.1 is the same and is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.3 R.sub.4 wherein each of R.sub.3 and R.sub.4 is hydrogen or a lower alkyl group of from 1 to 4 carbon atoms and can be the same or different, or ##STR3## wherein R.sub.5 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; and pharmaceutically acceptable salts and individual optical isomers thereof.

Abstract: Compounds of the formula ##STR1## wherein R is (a) optionally-substituted and optionally-hydrogenated biphenylyl, (b) optionally-substituted and optionally-hydrogenated bicyclic aryl having from 8 to 12 ring carbon atoms or (c) a radical of the formula ##STR2## R.sup.1 is aliphatic hydrocarbyl, alicyclic hydrocarbyl or optionally-substituted phenyl;R.sup.2 is --H or lower aliphatic hydrocarbyl;R.sup.3 is --H, lower alkyl, cycloalkyl, optionally-substituted phenyl or, with R.sup.4, alkylene;R.sup.4 is lower alkyl, cycloalkyl, optionally-substituted phenyl, optionally-(nuclearly)-substituted phenalkyl or, with R.sup.3, alkylene;or R.sup.2,R.sup.3 and R.sup.4, together with the carbon to which each is bound, are adamantyl; andn is 3, 4 or 5;and salts thereof with a base are pharmacologically active. Esters thereof are valuable intermediates for the preparation of the pharmacologically-active compounds. Physiologically-acceptable embodiments are administered, e.g.

Abstract: A process for the chemical catalytic hydrolysis of an .alpha.-aminonitrile or of one of the salts thereof, characterized in that an aqueous solution containing at least one carbonyl derivative is reacted with the said .alpha.-amine nitrile or with one of the salts thereof in the presence of hydroxide ions.

Abstract: Optically active 2-amino-2-phenylacetic acid of the formula ##STR1## in which R.sub.1, R.sub.2 and R.sub.3, which are identical or different, denote hydrogen, halogen, hydroxy, alkyl, acyl, or alkoxy, is prepared by asymmetrical transformation of a corresponding DL-aminophenylacetonitrile with L(+)-tartaric acid. To this end the corresponding DL-2-amino-2-phenyl-acetonitrile is reacted with approximately equimolar amounts of L(+)-tartaric acid in the presence of at least one alkanol having from 1 to 5 carbon atoms and/or at least one carbonyl compound at a temperature of from 0.degree. to 50.degree. C. and the mixture is stirred for 2 to 120 hours at the indicated temperature. The crystallized transformation product is separated, hydrolyzed by treatment with an acid and the desired product is isolated.

Abstract: New carboxyalkylacylamino acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.

Abstract: New optically active bis phosphine compounds which are usful in optically active catalysts. Such catalysts are particularly useful in catalytic asymmetric hydrogenation.

Abstract: A process is disclosed for the separation of a mixture of an optically active .alpha.-phenylglycine amide and the corresponding optically active .alpha.-phenylglycine acid, through the formation of a novel Schiff base of at least the amide, and achieving the separation with the resulting solubility differences while substantially completely avoiding racemization.

Abstract: Novel substituted aromatic aliphatic amino carboxylic acids containing a tertiary nitrogen atom such as 3-[N-ethyl-[1-methyl-2-(4-methoxyphenyl)] ethylamino] -1-propane carboxylic acid ethyl ester or 7-[N-ethyl-[1-methyl-2-(4-methoxyphenyl)] ethylamino] -1-heptane carboxylic acid ethyl ester have been found to be useful spasmolytic agents.

Abstract: The separation of constituents is carried out in such a way that a mixed amino acid sample is supplied to a separation column packed with a cation exchange resin and that, during the analysis of the single sample, five sorts of elutes of different compositions are supplied to the separation column in succession and by stages. The pH of the elute at the second stage is held higher than that of the elute at the first stage, and the pH's of the elutes at the third to fifth stages are held successively higher. However, the pH of the elute at the third stage is held lower than that of the elute at the second stage. On the other hand, the concentrations of counter ions contained in the elutes at the first to fifth stages are held successively higher inversely to the order in which the elutes are supplied. Notwithstanding that the pH of the elute at the third stage is lowered, the broadening of a component peak can be prevented by the increase of the counter ion concentration.