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: 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: Compounds of formula (I): ##STR1## wherein: X is CO, protected CO, CROH in which R is hydrogen or C.sub.1-4 alkyl and in which the OH moiety may be protected;Y is CH.sub.2 CH.sub.2 or CH.dbd.CH;Z is CO or CH.sub.2 ;n is 1 to 8;m is 1, 2 or 3;R.sub.1 is hydrogen, CH.sub.2 OH, CH.sub.2 OH in which the OH moiety is protected, CO.sub.2 W wherein W is hydrogen or CO.sub.2 W represents an ester group in which the ester moiety contains from 1 to 12 carbon atoms, or CONH.sub.2 ;R.sub.2 is hydrogen, C.sub.1-4 alkyl, or taken together with R.sub.3 and the carbon atom to which it is attached represents a carbonyl group;R.sub.3 is hydrogen, hydroxy or protected hydroxy;R.sub.4 is hydrogen or C.sub.1-9 alkyl;and salts thereof--have useful pharmacological properties.

Abstract: Compositions are disclosed having a physiological cooling action on the skin. The compositions contain, as the active ingredient, certain acyclic tertiary and secondary carboxamides.

Abstract: Described is a process for preparing hydrogenated derivatives of 2,6,6-trimethyl cyclohexene derivatives by means of treating said derivatives with hydrogen in the presence of a supported palladium catalyst such as palladium-on-calcium carbonate or palladium-on-barium sulfate in the presence of a quinoline activator. The resulting products are useful for their organoleptic properties as foodstuff flavorants and flavor enhancers, perfume composition ingredients, perfumed article ingredients and tobacco flavorants and flavor enhancers.

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 chiral .alpha.-amino acid having a hydrogen substituent in a position alpha to the carboxylic function thereof is prepared by subjecting a corresponding optical antipode with a chiral amino acid to a strong base whereby the proton in a position alpha to the carboxylic function is removed and thereafter reacting the resulting product with a chiral protonation agent.

Abstract: Disclosed is a process for the stereocontrolled total synthesis of thienamycin, which synthesis proceeds via intermediate II: ##STR1## wherein R.sup.5 and R.sup.6 are removable protecting groups.

Abstract: A compound of formula (I): ##STR1## wherein: A is >CH-- and n is 1 to 6; orA is >C.dbd.CH-- and n is 0 to 5; orA is >CH--CH.dbd.CH and n is 0 to 4; andR.sub.1 is hydrogen or C.sub.1-6 alkyl;R.sub.2 is hydrogen or C.sub.1-4 alkyl; andR.sub.3 is C.sub.4-9 alkyl, C.sub.5-7 cycloalkyl or C.sub.5-7 cycloalkyl-C.sub.1-6 alkyl; and salts thereof, has antiplatelet aggregation and bronchodilation activity.

Abstract: 1,2,3,4-Tetrahydro-1,5-benzodiazocines having the following formula ##STR1## in which R.sup.1 is a hydrogen, alkyl radical having at most 6 carbon atoms, methoxyethyl, or benzyl radical,R.sup.2 is a halo, hydroxyl, acetoxy or benzoxy radical,R.sup.3 is a phenyl, 2-methylphenyl, 2-chlorophenyl, 2-bromophenyl, 2-fluorophenyl, 2-nitrophenyl, 2-(trifluoromethyl)phenyl, 3-(trifluoromethyl)phenyl, 2,3-dichlorophenyl, 2,4-dichlorophenyl, 2,6-dichlorophenyl, 3,4-dichlorophenyl, 3,4-dimethoxyphenyl, or 3,4,5-trimethoxyphenyl radical,R.sup.4 is a hydrogen, chloro, fluoro, bromo, trifluoromethyl, methyl, methoxy, or methylthio radical, andR.sup.5 is a hydrogen or methoxy radical, or R.sup.4 and R.sup.5 together are an ethylendioxy radical, or an acid addition salt of the said benzodiazocine, and processes of making the same are described.

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: Disclosed are additives for hydrocarbon fuels which are the reaction products of a polyamine and an alkyl ester of acrylic or alkyl acrylic acid. A preferred composition is a mixture of the reaction product and oxygenated or non-oxygenated mono- or polyamines.

Abstract: The amino acid 2-amino-4-(2-aminoethoxy)-trans-but-3-enoic acid can be conveniently prepared via novel intermediates from a 2,2'-disubstituted diethyl ether and a dialkyl N-protected amidomalonate starting material using a multi-step process. Preferred starting materials are bis-2-chloroethyl ether and diethyl acetamidomalonate. The process, in a preferred embodiment, proceeds through the key intermediate ethyl-2-acetamido-4-[2-(2-phthalimido)ethoxy]-but-2-enoate.

Abstract: 3-Oxacaprolactam is prepared by a process which comprises: contacting an organic acid anhydride solution of a cyanoalkoxyalkanoate with hydrogen in the presence of a noble metal hydrogenation catalyst to prepare an amide-ester; and heating the amide-ester in excess water at a temperature above about 200.degree. C.

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

Abstract: Described is a process for augmenting or enhancing the aroma of a perfume composition as well as perfume and cologne compositions containing a mixture consisting essentially of compounds having the structures: ##STR1## and wherein the mixture contains 30% of the compounds having the structures; ##STR2## and 60% of the compound having the structure: ##STR3##

Abstract: The present invention is directed to compounds of the formula ##STR1## wherein R.sub.1 is lower alkyl and R.sub.2 is lower alkyl or aryl. Also provided are methods for preparation of these compounds. The compounds of formula I above are useful as plant growth regulants.

Abstract: Compounds of formula (I): ##STR1## wherein: m is 1 or 2; n is 4 to 8; X is CO, protected CO, or CROH wherein R is hydrogen or C.sub.1-4 alkyl and wherein the OH moiety may be protected; R.sub.1 is hydrogen or CO.sub.2 R.sub.1 represents an ester group in which the R.sub.1 moiety contains from 1 to 12 carbon atoms; R.sub.3 is hydroxy, or protected hydroxy; R.sub.2 and R.sub.4 are separately hydrogen, C.sub.1-9 alkyl, C.sub.5-8 cycloalkyl, C.sub.5-8 cycloalkyl-C.sub.1-6 alkyl, phenyl, phenyl C.sub.1-6 alkyl, naphthyl, naphthyl C.sub.1-6 alkyl, any of which phenyl or naphthyl moieties may be substituted by one or more halogen, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or nitro groups; or R.sub.2 and R.sub.4 taken with the carbon atom to which they are joined represent a C.sub.5-8 cycloalkyl group; and salts thereof; except that when one of R.sub.2 and R.sub.4 is hydrogen or C.sub.1-4 alkyl then the other of R.sub.2 and R.sub.4 cannot be hydrogen or C.sub.

Abstract: Catalytic asymmetric hydrogenation of a compound of the formula ##STR1## wherein R, R.sup.1 and R.sup.2 each independently represent hydrogen, substituted or unsubstituted alkyl having from 1 to 5 carbon atoms or substituted or unsubstituted aryl, and R.sup.3 represents substituted or unsubstituted alkyl having from 1 to 5 carbon atoms or substituted or unsubstituted aryl, provided that, if only one of R and R.sup.1 is hydrogen the Z geometric isomer is hydrogenated, in the presence of a homogeneous, coordination complex catalyst comprising rhodium, iridium or ruthenium in combination with an optically active bis phosphine ligand provides an excellent level of optical purity.

Abstract: Compounds of formula (I): ##STR1## wherein: n is 4 to 8, X is CO, protected CO or CROH wherein R is hydrogen or C.sub.1-4 alkyl and wherein the OH moiety may be protected; R.sub.1 is hydrogen, or CO.sub.2 R.sub.1 represents an ester group in which the R.sub.1 moiety contains from 1 to 12 carbon atoms; R.sub.3 is hydroxy or protected hydroxy; R.sub.2 and R.sub.4 are separately hydrogen, C.sub.1-9 alkyl, C.sub.5-8 cycloalkyl, C.sub.5-8 cycloalkyl-C.sub.1-6 alkyl, phenyl, phenyl C.sub.1-6 alkyl, naphthyl, naphthyl C.sub.1-6 alkyl, any of which phenyl or naphthyl moieties may be substituted by one or more halogen, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or nitro groups; or R.sub.2 and R.sub.4 taken with the carbon atom to which they are joined represent C.sub.5-8 cycloalkyl; A is hydrogen or a group CO.sub.2 B wherein B is hydrogen, or CO.sub.

Abstract: The invention relates to the testing of humans or other animals, for allergic reaction or hypersensitivity to penicillins. The tests can be used both to predict and to diagnose allergy. The invention comprises new penicilloyl-polylysine (PPL) preparations, new materials for use in minor determinant mixture (MDM) compositions and novel test methods employing such materials.The new PPL preparations comprise homogeneous, high purity, maximally coupled, .alpha.-diastereoisomeric, penicilloyl conjugates of low molecular weight PPLs. The PPL materials of the invention have the molecular structure in accordance with the following generic formula: ##STR1## wherein: R is selected from the group consisting of H and penicilloyl groups or similar groups derived from cephalosporins or other .beta.-lactam antibiotics; andn is an integer of from 4 to 10,at least about 66% and up to 100% of the R groups are other than hydrogen.

Abstract: Described is a process for preparing several 1-acyl-2,6,6-trimethylcyclohexene derivatives defined by the generic structure: ##STR1## wherein R.sub.1 is hydrogen or ethylidene having the structure:[H.sub.3 C--C.dbd. ;R.sub.2 is hydrogen or no group; one of the wavy lines is a carbon-carbon double bond and the other of the wavy lines is a carbon-carbon single bond; with the proviso that when the .DELTA..sup.2,3 bond (as shown by the wavy line between the "2" and the "3" position of the ring) is a carbon-carbon double bond, then R.sub.2 is hydrogen and R.sub.

Abstract: A compound of the formula: ##STR1## WHEREIN Q is a hydrogen atom, --CH.sub.2 CH(OH)CH.sub.2 Rf or a hydrocarbon residue having a valence corresponding to m which may contain one or more of --O--, --COO--, --NH--, --N.dbd. and ##STR2## IN THE CHAIN, R is a hydrogen atom, a hydrocarbon residue or --CH.sub.2 CH(OH)CH.sub.2 Rf and m is an integer of not less than 1, Rf being a perfluoroalkyl group, an .omega.-hydro-perfluoroalkyl group o an .differential.-chloro-erfluoroalkylgroup having 4 to 20 carbon atoms, which is useful as an agent for rendering fibrous materials oleophobic and anti-soiling and may be prepared by reacting a perfluoroalkylpropylene oxide of the formula: ##STR3## wherein Rf is the same as defined above, with a reagent of the formula:Q'(NHR').sub.mwherein Q' is a hydrogen atom or a hydrocarbon residue having a valence corresponding to m which may contain one or more of --O--, --COO--, --NH-- and --N.dbd.

Abstract: Novel ester diol alkoxylate acrylates prepared by the reaction of an ester diol and an alkylene oxide to produce an ester diol alkoxylate that is subsequently reacted with acrylic acid or methacrylic acid. The novel derivatives are useful as vehicles in coating and ink compositions and as monomers in the production of polymers.

Abstract: Novel ester diol alkoxylates produced by the reaction of an ester diol and an alkylene oxide. The reaction product is a vehicle useful in ink or paint formulations, as a solvent, and in adhesive formulations; it is also useful as an intermediate in the production of other valuable compounds and as a surfactant.

Abstract: Certain N-(2-hydroxyalkyl) derivatives of N-phosphonomethylglycine have been found to be useful as herbicides for the treatment of undesired plants.

Abstract: A compound of the formula ##STR1## wherein R.sub.1 is lower alkyl, aryloxy(lower)alkyl or ar(lower)alkyl,R.sub.2 is lower alkyl,Coor.sub.3 is esterified carboxy selected from lower alkoxycarbonyl and ar(lower)alkoxycarbonyl,X is halogen selected from bromine and chlorine, andX' is hydrogen or halogen selected from bromine and chlorine,Said aryl and said ar each constituting phenyl, tolyl or xylyl, and a method of making it are disclosed.

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

Abstract: Carboxyalkylureido cephalosporins of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen or methoxy; A is straight or branched chain alkylene of 1 to 6 carbons; R.sub.2 is hydrogen, lower alkyl, phenyl, phenyl-lower alkyl, diphenyl-lower alkyl, alkali metal ion or alkaline earth metal ion; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.5 is hydrogen or lower alkyl; R.sub.6 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR3## or certain heterothio groups; are disclosed. These compounds are useful as antibacterial agents.

Abstract: Novel imide carboxylates, O-carboxylates thereof, and amide carboxylates are useful as intermediates for preparation of sequestrant compounds.

Abstract: Novel imide carboxylates, O-carboxylates thereof, and amide carboxylates are useful as intermediates for preparation of sequestrant compounds.

Abstract: This invention relates to 10-aza-11,12-secoprostaglandins and processes for their manufacture. These compounds have prostaglandin-like biological activity and are particularly useful as renal vasodilators.

Abstract: Novel N-substituted amino acid derivatives of the formula: ##STR1## wherein R.sub.1 is an alkenyl group having 2 to 5 carbon atoms, a halogen-substituted alkenyl group having 2 to 5 carbon atoms or an alkynyl group having 2 to 5 carbon atoms, R.sub.2 is a methyl or ##STR2## group in which R.sub.2 ' is an alkyl group having 1 to 4 carbon atoms or a halogen-substituted alkyl group having 1 to 4 carbon atoms; and R.sub.3 is a hydrogen atom, an alkyl having 1 to 20 carbon atoms, cycloalkyl having 3 to 6 carbon atoms, benzyl, hydroxyethyl or methoxyethyl group, and inorganic or organic acid addition salts thereof, which possess useful soil fungicidal activities and can be produced by reacting a sarcosine derivative of the formula:CH.sub.3 HNCH.sub.2 COOR.sub.3 (II)wherein R.sub.3 is as defined above, with a halogen compound of the formula:R.sub.1 -- X (III)wherein R.sub.1 is as defined above and X is a halogen atom, or by reacting an N-substituted glycine derivative of the formula: ##STR3## wherein R.sub.1 and R.

Abstract: Certain N-(2-hydroxyalkyl) derivatives of N-phosphonomethylglycine have been found to be useful as herbicides for the treatment of undesired plants.