Abstract: High molecular weight amines having reduced low molecular weight amine contents are obtained by reacting a mixture of (1) a high molecular weight amine and (2) a low molecular weight amine with (3) an isocyanate in quantities such that from 0.5 to 10 equivalents of isocyanate are present for each equivalent of low molecular weight amine. The product of high molecular weight amines is particularly useful in the production of isocyanate addition products such as polyurethane plastics and foams.

Abstract: The present invention provides a lipase substrate of the general formula: ##STR1## wherein A is an alkylene or alkenylene radical containing up to 16 carbon atoms, R and R.sub.1, which can be the same or different, each signify an alkyl, alkenyl or acyl radical containing up to 20 carbon atoms or an optionally alkyl-substituted aryl or aralkyl radical containing up to 8 carbon atoms in the alkyl moiety and wherein one of R and R.sub.1 can also be a hydrogen atom, X is the residue of an aromatic hydroxy or thiol compound, and each Y and Z, independently from each other, is --S-- or --O--, Z also --CH.sub.2 --.The present invention also provides a process and a reagent for the optical determination of lipase.

Abstract: 2,3-Dihydro-1H-pyrrolo[1,2-a]pyrrole-1,7-dicarboxylates of the formula, ##STR1## in which each R is independently H or lower alkyl, are prepared from di(lower alkyl) 1,3-acetone-dicarboxylates.

Abstract: Liquid coating compositions adapted to be cured by exposure to ionizing radiation are disclosed in which a liquid vehicle of coating viscosity having an ethylenically unsaturated portion comprising one or more polyethylenically unsaturated materials adapted to cure on radiation exposure, pigment dispersed in the vehicle, and an acrylate-functional radiation-curable dispersant having free carboxyl group for wetting the pigment and assisting in the stable dispersion of the pigment in the vehicle. This dispersant is an acrylate-functional carboxylic acid amide carrying free carboxyl groups, especially an adduct of a polyacrylate and a stoichiometric deficiency of a primary amine to provide a secondary amine having acrylate functionality, the secondary amine functionality being reacted with a polycarboxylic acid anhydride to form amide groups therewith.

Abstract: 3.beta.-Substituted succinimido)azetidinones represented by the formula ##STR1## wherein R and R.sub.1 are e.g. C.sub.1 -C.sub.5 alkanoyloxy, benzoyloxy, substituted benzoyloxy, or benzyloxy, or one of R and R.sub.1 is hydrogen and the other is as defined above; R.sub.2 is C.sub.1 -C.sub.4 alkoxycarbonyl or an arylvinyl group e.g. styrryl or 2-furylvinyl; and R.sub.3 is e.g. protected-carboxymethyl, or an NH protecting group; are provided via stereoselective cycloaddition of imines with chiral auxiliary 3,4-disubstituted succinimidoacetyl chlorides. The chiral auxiliary e.g., 3S,4S-dibenzoyloxy-and 3S,4S-diacetoxysuccinimidoacetyl chloride, is obtained from tartaric acid via anhydride and imide formation with retention of chirality. The chiral azetidinones obtained are useful intermediates to .beta.-lactam antibacterial compounds.

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: A process for the synthesis of glutamic acid intermediate from an acrylate, amide and syngas by reacting them in the presence of a catalyst comprising a cobalt-containing compound, a bis-phosphine ligand and a solvent at a pressure of at least 500 psi and a temperature of at least 50.degree. C. and thereafter extracting the glutamic acid.

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: In the process for the preparation of 4-benzyl aspartate starting from dibenzyl aspartate and/or its salts only one benzyl group is selectively removed by catalytic hydrogenation. By setting up appropriate reaction conditions elimination takes place mainly of the benzyl group on the C.sub.1 atom of the compound. The desired product can be isolated from the reaction mixture by precipitation.

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 novel class of compounds has been found to be effective in blocking cholesterol and neutral lipid synthesis in-vivo without adversely affecting energy metabolism, useful for the treatment of obesity, hyperlipidemia and maturity-onset diabetes. The active compounds have the general formula ##STR1## or in-vivo hydrolyzable functional derivatives of the carboxylic groups thereof,whereinR.sub.1 and R.sub.2 each independently represents an unsubstituted or substituted hydrocarbyl or hetercyclyl radical;X and Y each independently represents hydrogen, optionally substituted lower alkyl, halogen, cyano, carboxy, lower alkoxycarbonyl or carbamoyl; andQ represents a diradical consisting of a linear chain of 8 to 14 carbon atoms, one or more of which may be replaced by heteroatoms, said chain being optionally substituted by inert substituents and one or more of said carbon or heteratom chain members optionally forming part of a ring structure.

Abstract: R-(Z)-4-amino-3-chloro-2-pentenedioic acid is a novel antibacterial and isolated from Streptomyces viridogenes MA5450, ATCC 39387.

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

Abstract: Water-soluble zwitterionic compounds having clay soil removal/anti-redeposition properties. The zwitterionic compounds are selected from monozwitterionic compounds, dizwitterionic compounds, polyzwitterionic compounds, and zwitterionic polymers. These zwitterionic compounds are useful in detergent compositions at from about 0.05 to about 95% by weight. In addition to the zwitterionic compounds, the detergent compositions further comprise from about 1 to about 75% by weight of a nonionic, anionic, ampholytic, zwitterionic, or cationic detergent surfactant or mixture thereof.

Abstract: Ethylenically unsaturated monomers containing activated ester groups are used to make polymers and copolymers which are useful in coatings, adhesives and moldings.

Abstract: A phenol derivative represented by the formula ##STR1## wherein R.sup.1 is a secondary or tertiary hydrocarbon residue of having 3 to 8 carbon atoms, R.sup.2 is a hydrocarbon residue having 1 to 12 carbon atoms, X is ##STR2## wherein R.sup.3, R.sup.4 and R.sup.5 each is an alkylene group having 1 to 4 carbon atoms, Z is an n-valent group and n is an integer of 1 to 8.This compound is effective to prevent the oxidation of organic materials.

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: Process for preparing diesterdiamides, consisting of reacting a diester with a diamine under wet conditions in the presence of suitable solvents and catalysts, to give the diester diamide, together with an ester salt derivative as impurity. The reaction product is then filtered to give a diesterdiamide cake and a mother solution of the reagents which also contains the solvent, the catalyst and the ester salt product. The cake is washed with a solvent of the ester salt, which also dissolves the reagents and catalysts. The mother solution and wash solution are then distilled, the two fractions obtained being recycled to the synthesis and to the wash.

Abstract: Amino-polyacetic acids such as ethylenediaminetetraacetic acid, diethylene triaminepentaacetic acid and nitrilotriacetic acid are reacted with alkanols and then with hydrazine to form the hydrazides which may be converted to carboxyhydrazides, i.e. carbazic acids. The products perform well as chelants and sequestering agents.

Abstract: Nonvolatile plasticizers are provided which are the carboxyl-functional amide reaction product of: (1) a secondary amine-functional adduct of an acrylate compound, like 2-hydroxyethyl acrylate or a monohydric caprolactone monoacrylate, and about one amine equivalent per acrylate group in the acrylate compound, of an organic primary amine such as a polyoxypropylene monoprimary amine having a molecular weight in the range of about 50 to about 8000; with (2) a dicarboxylic acid anhydride, like phthalic anhydride. These plasticizers have improved wetting properties and are particularly useful in nitrocellulose compositions, such as nail polish.

Abstract: This application relates to a stereospecific process for preparing specific enantiomers of 4-amino-4,5-dihydro-2-furancarboxylic acid and C.sub.1-6 lower alkyl esters thereof. These compounds are .gamma.-aminobutyric acid transaminase inhibitors useful in the treatment of epilepsy.

Abstract: The invention relates to compounds possessing GABA-like sedative and tranquilizing activity, characterized by being of general formula:X.sub.1 OC--(CH.sub.2).sub.2 --NH--(CH.sub.2).sub.3 --CO--X.sub.2whereX.sub.1 and X.sub.2 are hydroxyl, a C.sub.1 -C.sub.6 alkoxy group or a free or substituted amino group, X.sub.1 being the same as or different from X.sub.2.The invention also relates to processes for their preparation, and composition for pharmaceutical and veterinary use which contains them.

Abstract: Dense star polymers having terminal group densities greater than conventional star polymers exhibit greater and more uniform reactivity than their corresponding conventional star polymers. For example, a third generation, amine-terminated polyamidoamine dense star polymer prepared from ammonia, methyl acrylate and ethylenediamine has 1.24.times.10.sup.-4 amine moieties per unit volume (cubic Angstrom units) in contrast to the 1.58.times.10.sup.-6 amine moieties per unit volume contained by a conventional star polymer. Such dense star polymers are useful as demulsifiers for oil/water emulsions, wet strength agents in the manufacture of paper, and agents for modifying viscosity in aqueous formulations such as paints.

Abstract: A process for preparing phosphonomethylated amino acids comprising phosphonomethylating an N-carbamylated amino acid derivative with formaldehyde and a phosphorus source to obtain a phosphonomethylated N-carbamylated amino acid derivative which is then hydrolyzed to the corresponding phosphonomethylated amino acid, e.g. glyphosate, or acid derivative.

Abstract: The invention relates to compounds and salts of compounds which are diaminopimelyl peptides, N-acetoxypropionyl or N-t-butoxycarbonyl-amino-acid - (.alpha.-OBzl) glutamic acid peptides or N-acylated derivatives of (.alpha.-OBzl) glytamic acid or of (.alpha.-OBzl) aminoadipic acid.The compounds and their salts are starting materials for the preparation of pharmacologically active peptides.

Abstract: Prepare 4-amino-1,3-dicyano-2-methyl-1,3-pentadiene and related substituted aminodienes by contacting .beta.-aminocrotononitrile and related substituted aminoalkenes with a base acceptor in a solvent under mild conditions.

Abstract: N-acyliminodiacetic acids are manufactured by reacting formaldehyde or a formaldehyde generator compound with a N-unsubstituted amide or a generator thereof and with carbon monoxide in contact with a carbonylation catalyst, for example, a cobalt compound, the ratio of the aldehyde groups to the amide groups being at least 2:1. The formaldehyde generator can be a polymeric form of formaldehyde and the amide generator can be a carboxylic ester, acid or anhydride.

Abstract: A process for preparing phosphonomethylated amino acids comprising phosphonomethylating an N-carbamylated amino acid derivative with formaldehyde and a phosphorus source to obtain a phosphonomethylated N-carbamylated amino acid derivative which is then hydrolyzed to the corresponding phosphonomethylated amino acid, e.g. glyphosate, or acid derivative.

Abstract: For the preparation of polyfunctional organic compounds having at least one functional group of medium nucleophilic character selectively blocked by a tertiary butyl group, the corresponding unblocked compound is dissolved in a solution of concentrated sulfuric acid in an organic ether, and excess liquid isobutene is added to the solution at a temperature of not more than 5.degree. C.

Abstract: A process for preparing phosphonomethylated amino acids comprising phosphonomethylating a N-carboxymethyl-S-methylene bisdithiocarbamate with formaldehyde and a phosphorus source to obtain a phosphonomethylated bisdithiocarbamate which is then hydrolyzed to the phosphonomethylated amino acid salt. Acidification yields the corresponding phosphonomethylated amino acid, e.g. glyphosate, or acid derivative.

Abstract: Novel acyl-derivatives of the .beta.-hydroxy-.gamma.-butyrobetaine are disclosed (typically pyruvyl carnitine hydrochloride) which are useful therapeutic agents in the treatment of cardiac disorders, hyperlipidoemias and hyperlipoproteinemias.

Abstract: A sulfonic acid salt of an acyloxyalkylamine is prepared by reaction of an organic acid or amino-acid with a sulfonic acid salt of an alkanolamine. Isocyanates are prepared therefrom by reaction with phosgene.

Abstract: Disclosed is a process for preparing (2S)-tetrahydro-2.alpha.-methyl-6-oxo-4.beta.-amino-2H-pyran-3.alpha.-carb oxylic acid (I) which is useful in the synthesis of thienamycin. The process proceeds via a stereospecific reduction of the 2-acetyl-3-(R)-.alpha.-methylbenzylamino-2-pentenedioic acid diester (II). ##STR1## wherein R is, .alpha.-methylbenzyl, and R.sup.1 is lower alkyl having 1-6 carbon atoms or arylalkyl such as benzyl.

Abstract: A process for preparing .alpha.-amino acids or ester thereof having an .alpha.-vinyl substituent and certain intermediates are disclosed.

Abstract: Dimethacrylates are provided having the following chemical structure: ##STR1## where n represents a number of 2 to 8;R.sub.1 and R.sub.2 are the same or different and are hydrogen or groups of the formula: ##STR2## where R.sub.3 is an aliphatic, aromatic or cycloaliphatic group having 1 to 14 carbon atoms. These compounds are useful in dental material which cures to form polymers having high mechanical strength, low water sorption, resistance to staining, good color stability when exposed to short-wave radiation (e.g., sunlight) and good chemical resistance to the oral environment. Also provided are a method for polymerizing these compounds in situ on teeth and a tooth comprising polymers of these compounds.

Abstract: New homopolymerizable or copolymerizable 3,3-disubstituted furan dione compounds are described of the formula ##STR1## wherein X is a reactive moiety and Y and R are unreactive moieties.

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

Abstract: .alpha.-[4-(4-Trifluoromethylphenoxy)phenoxy]alkanecarboxylic acids (the "4-trifluoromethylphenoxy group" of which may contain one chlorine atom as a substituent) and derivatives thereof useful as a herbicide, a herbicidal composition containing the compound, methods of controlling weeds and production thereof.

Abstract: Novel, transient prodrug forms of the phenolic dihydroxy sympathomimetic amines have (i) the structural formula (I): ##STR1## wherein X is O, S or NR.sup.5 ; n is 1 or 2; R.sup.1 is the monodehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 1, and the didehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 2; R.sup.

Abstract: Muconic acid monoesters of alkanediols of 2-6 carbons and of phenol are prepared by copper (II) oxidative cleavage of phenols, catechols or orthobenzoquinones. The products are useful as comonomers in polyamides and other polymers. The alkanediol or phenol is introduced into the copper (II) reactant or catalyst.

Abstract: Novel, transient prodrug forms of dopa and dopamine have (i) the structural formula (I): ##STR1## wherein each R is independently selected from the group consisting of hydrogen, R.sup.3 -CO- and ##STR2## wherein X is O, S or NR.sup.6 ; R.sup.1 is hydrogen or --COOR.sup.8 ; R.sup.2 is hydrogen or OR; R.sup.

Abstract: Disclosed is a process for the stereocontrolled total synthesis of thienamycin, which synthesis proceeds via intermediate II: ##STR1## wherein R is a readily removable carboxyl protecting group; and ##STR2## is a readily removable acyl group.

Abstract: Radiation polymerizable acrylyloxy-containing reaction products are provided from Michael addition reaction of an amide acrylate material with a primary or secondary amine. The resulting amine adducts of the amide acrylate compounds possess high cure rates in air.

Abstract: Disclosed is a process for the stereocontrolled total synthesis of thienamycin, which synthesis proceeds via intermediate II: ##STR1## wherein R.sup.3 is a readily removable carboxyl protecting group.

Abstract: A process for preparing .alpha.-amino acids or ester thereof having an .alpha.-vinyl substituent and certain intermediates are disclosed.

Abstract: N-(Phosphonoacetyl)-L-aspartic acid (PALA) compounds, especially novel PALA compounds, and methods for their preparation in large amounts are disclosed. These methods include preparation of certain PALA compounds such as PALA dibenzyl ester, disodium PALA, and the cyclohexylamine salt of dibenzyl PALA.

Abstract: A N-acyl .alpha.-amino acid is manufactured by reacting an unsaturated vegetable oil or a C.sub.8 -C.sub.30 mono-olefinic compound with an amide, carbon monoxide and hydrogen, in the presence of a cobalt catalyst. The process is operated in one step, providing for an increased selectivity as compared with a two-step process.

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: Adducts of alkylphosphorous triamides with alpha, beta-unsaturated carbonyl compounds provide novel sulfur-free load-carrying additives for various organic compositions, e.g., lubricant oils.