Abstract: New process for the synthesis of optically active aminoacids of formula ##STR1## by treating compounds of formula ##STR2## which an optically active alcohol of formulaR.sub.4 --OH (III)d or 1To obtain a pair of diastereoiosmer esters of formula ##STR3## which is resolved in basic medium into the single diastereoisomer esters of formula ##STR4## from which the desired optically active aminoacid of formula (I) is obtained by treatment in acid medium.

Abstract: Disclosed are some new aminoethylphosphinic acid derivatives useful as antibacterial agents.

Abstract: N-formyl amino acid or peptide is deformylated by reaction with aniline or methylene dianiline over noble metal catalyst, e.g., Pt-on-carbon. N-formanilide is formed as by-product. The process is particularly useful in deformylating N-formyl aspartame.

Abstract: Compounds of formula ##STR1## (wherein R, R.sub.1, R.sub.2 and X have the meanings reported in the specification), the processes for their preparation and the pharmaceutical compositions containing them as active ingredient are described.The compounds of formula I are useful in the treatment of Parkinson's disease, renal failure, cardiac decompensation and hypertension.

Abstract: A method for crystallizing alpha-L-aspartyl-L-phenylalanine methyl ester (APM) is disclosed. The APM is crystallized from a C.sub.1 -C.sub.3 -alcohol/water solution (30-80:70-20 (v/v)). The ester crystallized by (i) concentrating the solution, (ii) cooling the solution, (iii) adjusting the water:alcohol ratio, or (iv) a combination thereof.

Abstract: The invention relates to the preparation of water-soluble L-tyrosine derivatives having the formula ##STR1## where R.sub.1 is a L-malyl, L-lactyl, L-glutamyl or L-aspartyl group, R.sub.2 is a --OH, --OM, methoxy, ethoxy or amino group and M is an alkaline metal, by enzymatic condensation of an acid selected among L-malic, L-lactic, L-glutamic and L-aspartic acids, with a L-tyrosine derivatives selected among the ethyl and methyl esters and the amide of L-tyrosine. The enzyme is obtained from a culture of Micrococcus casealyticus. The compounds where R.sub.1 is a L-malyl or L-lactyl group are new. Said L-tyrosine derivatives are useful in cosmetic and pharmaceutical compositions, such as tanning and sun compositions.

Abstract: In the process of hydrocarboxylating an .alpha.-enamide with CO and H.sub.2 O or an organic hydroxyl compound to produce an N-acyl-.alpha.-amino acid or ester, respectively, the improvement comprising using as the .alpha.-enamide reactant, an .alpha.-enamide which has a chiral center that is essentially all L or D, thereby producing a reaction mixture containing diastereomeric N-acyl-.alpha.-amino acids or esters having two chiral centers, said mixture having essentially no enantiomeric pairs.

Abstract: The compound N-[(1S,2R)-fluoromethyl-2-hydroxy-2-(4-methylsulphonyl-phenyl)-ethyl]-2-pr openamide and the derivatives thereof in which the hydroxy in 2 position is esterified by a mono or dicarboxylic acid or by an aminoacid are described.Such compounds have antibiotic activity and are useful in human and veterinary therapy.

Abstract: Crystalline salts of (R,S)-pivaloyloxyethyl esters of (S)-3-(3,4-dihydroxyphenyl)-2-methylalanine, processes for their preparation and pharmaceutical composition are disclosed.

Abstract: Alkylphosphate solvents are disclosed for use in an amino acid and amino acid ester enzymatic coupling process. .alpha.-Aspartylphenylalanine methyl ester and intermediates thereof are prepared enzymatically in an alkylphosphate solvent or cosolvent.

Abstract: A process for making 2,6-disubstituted tyrosine by the noble metal coupling of a disubstituted aromatic halide or diazonium salt with an amino-protected 2-aminoacrylic acid to form a (Z)-.beta.-(disubstituted phenyl)-.alpha.-acylaminoacrylate, and asymmetrically hydrogenating the acrylate to produce the 2,6-disubstituted tyrosine.

Abstract: The present invention is directed to novel taxols useful as a chemotherapeutic agent. Moreover, the present invention is directed to the process of preparing taxols and various intermediates in said process. A key intermediate is this process is 2,5-dihydroxy-2-patchoulenes. Therefore the present invention is also related to said intermediate and the process for its preparation.

Abstract: Synthesis of phenylserine ester (a) via benzaldehyde and glycine ester using serine hydroxymethyltransferase; and (b) via methyl benzoylacetate. Synthesis of hydroxy-aspartame or derivative by enzymatic coupling of phenylserine or derivative with aspartic acid or derivative. Hydrogenation of the coupled product to give as final product aspartame or analog with related processes and products.

Abstract: This invention relates to chemical compounds which have selective thyromimetic activity. A compound of this invention is 3,5-dibromo-3'-[6-oxo-3(1H)-pyridazinyl-methyl]-thyronine.

Abstract: The invention relates to novel thyronine derivatives of the formula ##STR1## in which n is 10-400, R denotes H, alkyl or N-carbonylthyronine, R.sup.1 and R.sup.2 are identical or different and denote hydrogen or iodine, and R.sup.3 denotes H or alkyl, a process for the preparation of the compounds, and their use when carrying out immunoassays.

Abstract: A compound of D-phenylalanine derivative for hypoglycemic use, represented by the general formula ##STR1## R.sup.1 is selected from hydrogen, alkyl of 1 to 5 carbon atoms, aryl of 6 to 12 carbon atoms, aralkyl of 6 to 12 carbon atoms, ##STR2## --CH.sub.2 CO.sub.2 R.sup.3, --CH(CH.sub.3)--OCO--R.sup.3, and --CH.sub.2 --OCO--C(CH.sub.3).sub.3 ; R.sup.2 is selected from groups comprising aryl of 6 to 12 carbon atoms, a hetero six-membered ring, a hetero five-membered ring, cycloalkyl, or cycloalkenyl, any of which groups may have one or more substituents; and R.sup.3 is selected from hydrogen and alkyl of 1 to 5 carbon atoms; the salts thereof, and precursors which can be converted thereto in the human or animal body.Some of the compounds are novel per se.

Abstract: Synthesis of phenylserine ester (a) via benzaldehyde and glycine ester using serine hydroxymethyltransferase; and (b) via methyl benzoylacetate. Synthesis of hydroxy-aspartame or derivative by enzymatic coupling of phenylserine or derivative with aspartic acid or derivative. Hydrogenation of the coupled product to give as final product aspartame or analog with related processes and products.

Abstract: This invention relates to an improved process for preparing .alpha.-L-aspartyl-L-phenylalanine methyl ester. More specifically, it relates to a process for preparing .alpha.-L-aspartyl-L-phenylalanine methyl ester which comprises treating, as a raw material, N-formyl-.alpha.-L-aspartyl-L-phenylalanine in methanol in the presence of an acid to form .alpha.-L-aspartyl-L-phenylalanine dimethyl ester, hydrolyzing the .alpha.-L-aspartyl-L-phenylalanine dimethyl ester by bringing it into contact with hydrochloric acid in the presence of methanol as desired, separating the thereby-precipitated .alpha.-L-aspartyl-L-phenylalanine methyl ester hydrochloride and neutralizing the hydrochloride. Further, this invention also provides a process for preparing .alpha.-L-aspartyl-L-phenylalanine methyl ester capable of using, as a raw material, N-formyl-.alpha.-L-aspartyl-L-phenylalanine which contains N-formyl-.beta.-L-aspartyl-L-phenylalanine in an amount of 30% by weight or less.

Abstract: There are provided paraethylamine phenol compounds of formula I, ##STR1## and pharmaceutically acceptable derivatives thereof. There are also described the use of the compounds of formula I as pharmaceuticals, methods for making the compounds and pharmaceutical, e.g. cardiac, compositions containing the compounds.

Abstract: A 6-keto-prostaglandin E.sub.1 derivative of the formula: ##STR1## (wherein R.sup.1 represents an amino acid or amino alcohol residue, R.sup.2 represents a single bond or an alkylene group of from 1 to 4 carbon atoms, R.sup.3 represents (i) an alkyl group of from 1 to 8 carbon atoms, (ii) a cycloalkyl group of from 4 to 7 carbon atoms, which may be unsubstituted or substituted by at least one alkyl group of from 1 to 8 carbon atoms or (iii) a phenyl or phenoxy group, which may be unsubstituted or substituted by chlorine, trifluoromethyl or alkyl of from 1 to 3 carbon atoms, provided that when R.sup.2 represents a single bond R.sup.3 does not represent phenoxy)cyclodextrin clathrates thereof and non-toxic salts thereof possess selective cytoprotective activity.

Abstract: Disclosed herein is a process for preparing .alpha.-L-aspartyl-L-phenylalanine methyl ester or its hydrochloride from 5-benzyl-3,6-dioxo-2-piperazine acetic acid or its methyl ester, prepared without using L-penylalanine methyl ester which involves problems in its stability, as a raw material. Specifically, the process comprises: bringing 5-benzyl-3,6-dioxo-2-piperazine acetic acid in the presence of methanol or 5-benzyl-3,6-dioxo-2-piperazine acetic acid methyl ester in the presence or absence of methanol into contact with hydrochloric acid; isolating the thereby deposited .alpha.-L-aspartyl-L-phenylalanine methyl ester hydrochloride; and neutralizing said hydrochloride with an alkali as required. Preparation processes of 5-benzyl-3,6-dioxo-2-piperazine acetic acid or its methyl ester are also disclosed.

Abstract: The present invention relates to a process for preparing .alpha.-L-aspartyl-L-phenylalanine methyl ester or its hydrochloride. .alpha.-L-aspartyl-L-phenylalanine methyl ester or its hydrochloride is prepared by a process comprising: condensating N-formyl-L-aspartic acid anhydride and L-phenylalanine in water or in water containing methanol at a pH in the range of 7-12 to form N-formyl-.alpha.-L-aspartyl-L-phenylalanine; acidifying the reaction mixture successively with hydrochloric acid in the presence of methanol without isolating the N-formyl-.alpha.-L-aspartyl-L-phenylalanine so as to bring it into contact with hydrochloric acid in the presence of methanol for reaction and thereby to deposit .alpha.-L-aspartyl-L-phenylalanine methyl ester hydrochloride; separating the .alpha.-L-aspartyl-L-phenylalanine methyl ester hydrochloride; and neutralizing said hydrochloride as required.

Abstract: A process for preparing an .alpha.-L-aspartyl-L-phenylalanine methyl ester which comprises the steps of reacting formyl-L-aspartic anhydride with L-phenylalanine in the presence of water at a high pH, to produce formyl-.alpha.-L-aspartyl-L-phenylalanine; removing the formyl group from the formyl-.alpha.-L-aspartyl-L-phenylalanine and esterifying the resultant compound with methanol and hydrogen chloride to produce the hydrogen chloride salt of .alpha.-L-aspartyl-L-phenylalanine methyl ester; neutralizing the hydrogen chloride salt of .alpha.-L-aspartyl-L-phenylalanine methyl ester; and filtering the neutralized solution to produce .alpha.-L-aspartyl-L-phenylalanine methyl ester.

Abstract: This invention relates to an improved process for preparing N-formyl-.alpha.- aspartyl phenylalanine. More specifically, it relates to a process for preparing N-formyl-.alpha.-aspartyl phenylalanine by condensating N-formyl aspartic acid anhydride and phenylalanine which comprises effecting the condensation reaction in a water medium while maintaining the pH during the reaction in the range of 7-12 and at a reaction temperature of 50.degree. C. or below.

Abstract: The present invention relates to new compounds of the general formula: ##STR1## where X is iodine or hydrogen; A is a linking portion; and R is an iodinatable aryl or heteroaryl group having electron donating substituents. These compounds are useful precursors to the iodinated thyroid hormones for radioimmunoassay determination of thyroid hormones in biological fluids.

Abstract: Dipeptides containing C-terminal phosphinothricin of the formula ##STR1## in which phosphinothricin is attached to a--preferably natural--amino acids at the amino group are effective herbicides in the pre-emergence and post-emergence techniques. The compounds are obtained, for example, by reacting phosphinothricin with the hydroxysuccinimide ester of an amino acids which is protected at the amino group in the presence of a base and subsequently splitting off the protective groups.

Abstract: In the process of hydrocarboxylating an .alpha.-enamide with CO and an organic hydroxyl compound to produce a N-acyl-.alpha.-amino acid ester, the improvement comprising using as the organic hydroxyl compound reactant, an organic hydroxyl compound which has a chiral center that is essentially all L or D, thereby producing a reaction mixture having essentially no enantiomeric pairs and containing diastereomeric N-acyl-.alpha.-amino acid esters having two chiral centers.

Abstract: Compounds having the formula: ##STR1##are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory agents and cytoprotective agents.

Abstract: There is disclosed a process for the racemization of amino acids and derivatives thereof. The racemization process of the present invention uses an aromatic aldehyde-containing polymer made from the reaction of a hydroxy-aromatic aldehyde with a chloromethylated vinylbenzene polymer under reaction conditions to form an aromatic aldehyde-containing polymer wherein the aldehydic moiety is linked to the polymer through an ether linkage. There is also disclosed a process for the production of the racemization catalyst. Another embodiment of the invention comprises a process for the promotion of the racemization reaction wherein a tertiary amine-containing resin is used as a promoting agent.

Abstract: Synthesis of phenylserine ester (a) via benzaldehyde and glycine ester using serine hydroxymethyltransferase; and (b) via methyl benzoylacetate. Synthesis of hydroxy-aspertame or derivative by enzymatic coupling of phenylserine or derivative with aspertic acid or derivative. Hydrogenation of the coupled product to give as final product aspertame or analog with related processes and products.

Abstract: Novel substituted .alpha.-fluoromethyl-.alpha.-amino alkanoic acids and esters thereof are disclosed. The novel compounds have biological activity including decarboxylase inhibition.

Abstract: A process for producing .alpha.-L-aspartyl-L-phenylalanine methyl ester or its hydrochloride which comprises contacting N-formyl-.alpha.-L-aspartyl-L-phenylalanine methyl ester with a mixture of methanol and a highly concentrated hydrochloric acid at a temperature of between 0.degree. and 40.degree. C., whereby the amino-protecting formyl group is removed and .alpha.-L-aspartyl-L-phenylalanine methyl ester crystalizes, and isolating the hydrochloride crystals, and, if desired, converting the hydrochloride to free .alpha.-L-aspartyl-L-phenylalanine methyl ester, is disclosed along with variations thereof. The process is commerically advantageous in that it utilizes inexpensive materials while minimizing hydrolysis of the peptide bond.

Abstract: Prodrugs of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formula (I): ##STR1## the amido ester moiety of which is in the L-configuration, and pharmaceutically acceptable salts thereof are disclosed.

Abstract: A regioselective process for the preparation of .alpha.-L-aspartyl-L-phenylalanine methyl ester is disclosed. A controlled aqueous coupling reaction between .beta.-methyl-L-aspartate-N-carboxyanhydride and L-phenylalanine produces the aspartyl methyl ester of .alpha.-L-aspartyl-L-phenylalanine which is subsequently hydrolyzed and selectively esterified without isolation. The hydrochloride salt of .alpha.-L-aspartyl-L-phenylalanine methyl ester, which is selectively precipitated from the esterification mixture, can be neutralized to .alpha.-L-aspartyl-L-phenylalanine methyl ester.

Abstract: Crystalline salts of (R,S)-pivaloyloxyethyl esters of (S)-3-(3,4-dihydroxyphenyl)-2-methylalanine and processes for their preparation are disclosed.

Abstract: Novel .alpha.-allenic-.alpha.-amino acids which are enzyme inhibitors of the suicide or k.sub.cat type are disclosed herein.

Abstract: A simple single step process for preparing alkyl and substituted alkyl esters of amino acids is described. The products are bioactive compounds including compounds useful as antihypertensive agents.

Abstract: A new process for preparing alfa-L-aspartyl-L-phenylalanine alkyl esters of formula I ##STR1## wherein R represents an alkyl group having from 1 to 5 carbon atoms, starting from the corresponding alfa-haloacyl-alfa-L-aspartyl-L-phenylalanine alkyl esters.

Abstract: A process for preparing .alpha.-L-aspartyl-L-phenylalanine methyl ester consisting of:bringing N-formyl-L-aspartic anhydride and L-phenylalanine methyl ester, in a molar ratio equal or approximately equal to 1:1, into contact with a solid cation exchange resin having free sulphonic, phosphonic or carboxylic acid groups, the ration of the acid equivalents of said resin acid groups to the number of moles of the one or other reagent being equal to or less than about 1:1, and operating in the liquid phase in an inert organic solvent at a temperature of about 40.degree. C. or less, until a mixture of N-formyl-.alpha.-L-aspartyl-L-phenylalanine methyl ester and N-formyl-.beta.-L-aspartyl-L-phenylalanine methyl ester forms in which the .alpha. isomer prevails over the .beta. isomer;deformylating said N-formyl-.alpha.-L-aspartyl-L-phenylalanine methyl ester and N-formyl-.beta.-L-aspartyl-L-phenylalanine methyl ester; andseparating and recovering the .alpha.

Abstract: A process for producing .alpha.-L-aspartyl-L-phenylalanine methyl ester or its hydrohalide, which comprises subjecting 3-benzyl-6-carboxymethyl-2,5-diketopiperazine to partial hydrolysis with a strong acid in a solvent mixture of methanol and water.

Abstract: There are described new optically active 3,4-bis-(diphenylphosphino)-pyrrolidines of the formula ##STR1## wherein Ph is a phenyl group and R is hydrogen, an alkyl group, an arylalkyl group or an acyl group, rhodium complexes containing a compound of formula (I) as its chiral ligands, said rhodium complexes having the formula[RH(en).sub.2 A].sup.+ X.sup.- (II),where (en).sub.2 is two molecules of a monoolefin or one molecule of a diolefin, A is an optically active compound of formula (I) and X.sup.- is a tetrafluoroborate, hexafluorophosphate or a perchlorate ion, and use of the rhodium complexes as catalysts for the homogeneous asymmetric hydrogenation of unsubstituted or .beta.-substituted .alpha.-acylamino-acrylic acids.

Abstract: Amino acid ester hydrohalide is produced by reacting amino acid, alcohol, and halocarbonyl compound represented by the formula: ##STR1## in the presence of an excess of the alcohol and under substantially anhydrous conditions, wherein X.sub.1 and X.sub.2 are each independently fluoro, chloro, bromo, trichloromethoxy or tribromomethoxy.

Abstract: Compounds of the structure ##STR1## and pharmaceutically acceptable salts thereof, wherein: R.sub.1 and R.sub.2 are independently H, OH, lower alkyl, lower alkoxy, aryloxy, heteroaryloxy, heteroaryl lower alkoxy, aryl, heteroaryl, aryl-lower alkyl, aryl-lower alkoxy, halogenated aryl-lower alkoxy, lower alkenyl, lower alkynyl, lower alkenoxy, lower alkynoxy, halogen or trifluoromethyl;A is H, aryl, lower alkyl, aryl-lower alkyl or heteroaryl; andB is ##STR2## n=0-6, wherein D is H, CONR.sub.3 R.sub.4, CO.sub.2 H, CO.sub.2 R.sub.5, CH.sub.2 OH or CH.sub.2 OR.sub.6,whereinR.sub.3, R.sub.4, R.sub.5 and R.sub.6 are independently H, lower alkyl, aryl, aryl-lower alkyl or heteroaryl;E is H, OH, lower alkyl, aryl or heteroaryl; andF is ##STR3## wherein G is the same as R.sub.1 and R.sub.2, useful for the treatment of allergy, asthma and inflammatory conditions.

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: Novel radioactive stilbene derivatives marked with iodine 125 or 131 of the formula ##STR1## wherein each A and B are both hydrogen or together form a double bond and R is the remainder of amino acid of the formula R--NH.sub.2 or a derivative thereof possessing an iodine acceptor group and marked with iodine 125 or 131 and their preparation and antigens obtained therefrom and a process for preparing said antigens.

Abstract: Novel .alpha.-difluoromethyl tyrosines and esters thereof are disclosed. The novel compounds have useful pharmacological activity.

Abstract: New 3-N-acyl derivatives of 3-amino-2-hydroxy-4-phenylbutanoic acid are provided, which exhibit analgesic activity and are affective to enhance the morphine analgesia.

Abstract: A short-acting .beta.-blocking compound of the formula ##STR1## wherein Ar may be substituted or unsubstituted aromatic, Y may be a straight or branched carbon chain or aralkyl, R may be lower alkyl, lower alkenyl, lower alkynyl, aryl or aralkyl, and x is an integer from 1 to about 3; or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed is a crystalline form of diastereomeric L-.alpha.-methyldopa POE ester, also referred to as (R),(S)-.alpha.-pivaloyloxyethyl-(S)-3-(3,4-dihydroxyphenyl)-2-methylalani nate and a process for its isolation. Also disclosed is an improved process for the formation of diastereomeric L-.alpha.-methyldopa POE ester.

Abstract: The present invention relates to compounds of the formula ##STR1## wherein R' is hydrogen, straight or branched chain lower alkyl having from 1 to 4 carbon atoms or benzyl, Z is hydrogen or straight chain lower alkyl having from 1 to 4 carbon atoms, Y is hydrogen or a nitrogen blocking group selected from the group consisting of tertiary alkoxycarbonyl, benzyloxycarbonyl, cycloalkoxycarbonyl and vinyloxycarbonyl, R.sub.c is hydrogen, halogen or benzyloxy and R.sub.d is hydrogen, or R.sub.c and R.sub.d are benzyloxy; or an individual diastereomer thereof. Said compounds having use as intermediates in the production of enkephalin derivatives which in turn are used as analgesic and antipsychotic agents.