Abstract: A process for the preparation of activated esters of certain N-maleoyl amino acids is disclosed. In the process, maleamic acids are cyclized and esterified to the desired products by the initial reaction with an acid halide reagent followed by a subsequent reaction with the appropriate hydroxyl-containing compound. The activated esters of N-maleoyl amino acids are particularly suited for linking compounds containing an amino group with those containing a thiol group.

Abstract: A process for the preparation of an N-substituted unsaturated carboxylic acid amide represented by the following formula: ##STR1## wherein R.sup.1 means a hydrogen atom or methyl group Y denotes a methylene group, oxygen atom or methylimino group, m and n stand individually for an integer of 0 to 5, and m+n is an integer of 3 to 5. The process comprises reacting a specified .beta.-alkoxy-substituted carboxylate with a specified cyclic amine to form a .beta.-alkoxy-substituted carboxylic acid amide compound and then removing an alcohol from the carboxylic acid amide compound in the presence of a basic catalyst to form an unsaturated group.

Abstract: Fungicidal 1-aminomethyl-3-(2-fluoro-3-chlorophenyl)-4-cyano-pyrrole derivatives of the formula ##STR1## in which R stands for a ##STR2## wherein R.sup.1 stands for optionally substituted alkyl, for alkenyl, alkinyl or cycloalkyl, or for in each case optionally substituted aralkyl or aryl,R.sup.2 stands for in each case optionally substituted heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkinyl or heterocyclyl, for dialkylaminoalkyl or for in each case optionally substituted cycloalkylalkyl or phenethyl,R.sup.3 stands for hydrogen or alkyl andR.sup.4 stands for cyano, alkanoyl, alkoxycarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, for alkylsulphinyl, for alkylsulphonyl, for phenylsulphinyl or for phenylsulphonyl.The compound where R is replaced by an election-withdrawing leaving group is a novel intermediate.

Abstract: A process is described for the conversion of oxyalkylated alcohols to the corresponding alkoxylated tertiary amines, such as aminated ethoxylated amines, by reaction with a secondary amine at ambient pressure and at above ambient temperature in the presence of hydrogen and a reductive amination catalyst using, as a reductive amination catalyst, metallic iridium.

Abstract: The present invention is 2,3-methanoproline, derivatives thereof, and biologically active molecules incorporating 2,3-methanoproline. These compounds are useful as inhibitors of ethylene production in plant material, and as synthetic analogs of biologically active molecules.

Abstract: A guanidinobenzoic ester derivative having the formula is novel and effective to inhibit enzymes such as trypsin, plasmin and thrombin, being useful for treatment of the pancreatitis and hemorrhagic disease and thrombosis. ##STR1## wherein X represents a group of the formula: ##STR2## in which Y is a group of the formula: --(CH.sub.2).sub.m--, m being an integer of 2 or 3, ##STR3## or a group of the formula:--ORin which R is a hydrogen atom or a lower alkyl group, and n represents an integer of 1 to 5.

Abstract: Novel aminomethyloxooxazolidinyl arylbenzene derivatives, wherein the aryl includes the phenyl, substituted phenyl, pyridyl, and substituted pyridyl groups, such as (l)-N-{3-[4-(4'-pyridyl)phenyl]-2-oxooxazolidin-5-ylmethyl{acetamide, possess useful antibacterial activity.

Abstract: A method for preparation of polycyclic 1,3-thiazolidines is described. The method comprises reacting a fluoride ion source, in a solvent, with an onium salt synthesized by the reaction of a nitrogenous heteroaromatic compound with a halomethyl trimethylsilylmethyl sulfide, the halomethyl trimethylsilylmethyl sulfide being selected from the group consisting of chloromethyl trimethylsilylmethyl sulfide, bromomethyl trimethylsilylmethyl sulfide, or iodomethyl trimethylsilylmethyl sulfide.

Abstract: Novel homo bis-maleimide compounds containing sulfonate linkages are made by reacting an aromatic disulfonyl halide with m- or p-hydroxy phenyl maleimide and have the following formula: ##STR1## Similarly, co-bis-maleimides are made by reaching an aromatic disulfonyl halide, aromatic dihydroxy compound and m or p hydroxy phenyl maleimide having the structural formula: ##STR2## Herein R and R' are the same or different and are divalent radicals selected from the group consisting of meta arylene, para arylene, naphthalene and radicals of the formula A--A and A--Z--A wherein A is selected from the group consisting of meta arylene, para arylene and naphthalene and Z is selected from the group consisting of meta arylene, para arylene, naphthalene, carbonyl, sulfone, sulfide, sulfonyl, sulfonate, sulfoxide, ether, methylene, isopropyl, oxygen, alkyl, --CH.dbd.CH-- and --C.tbd.C-- and R.sub.1, R.sub.2, R.sub.3 and R.sub.

Abstract: Process for the industrial synthesis of (2S, 3 7aS)-2-carboxyperhydroindole by reduction of 2-carbox indole or of one of its esters to (R,S)-2-carboxyindo or of one of its esters which, after saponification, converted into the acid, the S isomer cf (R,S)-2-carboxyindoline being obtained by precipitation from the mixture of the two (R) and (S) isomers, in the presence of (+) methylbenzylamine, (S)-2-carboxyindoline being in its turn subjected to catalytic hydrogenation to give (2S, 3aS,7aS)-2-carboxyperhydroindole, after separation of (2S,3aR,7aR) isomer by crystallization.Application to the synthesis of carboxyalkyl d peptides capable of being employed in therapeutics.

Abstract: A 3-(substituted)-2-oxazolidinone is prepared by refluxing equimolar proportions of a dialkanolamine and dimethyl carbonate in the absence of a catalyst. A yield of at least about 90 percent of a highly pure product is obtained.

Abstract: Phenylalkenylcarboxylic acid and esters thereof of the general formula I ##STR1## where X is hydrogen or fluorine, R.sup.1 is hydrogen, C.sub.1 C.sub.6 -alkyl, C.sub.5 - or C.sub.6 -cycloalkyl, (C.sub.1 -C.sub.4 -alkoxy)-C.sub.2 -C.sub.4 -alkyl or (C.sub.1 -C.sub.4 -alkylthio)-C.sub.2 -C.sub.4 -alkyl; W is a divalent radical --CH.dbd.CR.sup.2 --; --CH.dbd.CY--; --CH.dbd.CR.sup.2 --CH.sub.2 --; --CH.dbd.CR.sup.2 --CH.dbd.CR.sup.3 -- or ##STR2## where Y is chlorine or bromine and R.sup.2 and R.sup.3 are each hydrogen or C.sub.1 -C.sub.4 -alkyl, with the proviso that X is not F when W is --CH.dbd.CR.sup.2 --, their manufacture, and their use as herbicides.

Abstract: The present invention relates to a method for the synthesis of certain bridged fused ring pyridines. Such bridged fused ring pyridines can be converted to huperzine A and analogs of huperzine A. The present invention also covers such bridged fused ring pyridines, compounds utilized for the preparation of the bridged fused ring pyridines and analogs of huperzine A.

Abstract: Benzo-fused cycloalkane and oxa- and thia-cycloalkane trans-1,2-diamine compounds of the formula: ##STR1## wherein A, B, C, D, n, X, Y, R, R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, e.g., trans-3,4-dichloro-N-methyl-N-[2-(pyrrolidin-1-yl)-5-methoxy-1,2,3,4-tetra hydronaphth-1-yl]benezeneacetamide, and the pharmaceutically acceptable salts or N-oxides thereof, are useful as analgesics and/or diuretics.

Abstract: N-Phenyltetrahydrophtalimides of the general formula I ##STR1## where R.sup.1 is hydrogen or halogen, R.sup.2 is halogen, R.sup.3 is hydrogen or C.sub.1 -C.sub.4 -alkyl, R.sup.4 is unsubstituted or C.sub.1 -C.sub.3 -alkoxy-substituted C.sub.1 -C.sub.8 -alkyl, C.sub.3 -C.sub.4 -alkenyl or C.sub.3 -C.sub.4 -alkynyl, and R.sup.5 is hydrogen or C.sub.1 -C.sub.4 - alkyl, methods for their manufacture, and their use as herbicides.

Abstract: Aminomethyl oxooxazolidinyl cycloalkylbenzene derivatives, such as l-N-[3-(2,3-dihydro-1-oxo-1H-inden-5-yl)-2-oxooxazolidin-5-ylmethyl]acetam ide, possess useful antibacterial activity.

Abstract: There are disclosed novel herbicidally active pyrrolidine-2,5-diones and 4,5,6,7-tetrahydroisoindolel,3-diones of formula ##STR1## wherein R.sup.1 is hydrogen; or C.sub.1 -C.sub.4 alkyl;R.sup.2 is C.sub.1 -C.sub.4 alkyl; orR.sup.1 and R.sup.2, when taken together, are a (CH.sub.2).sub.4 group which may be substituted by one or two C.sub.1 -C.sub.4 alkyl groups;X is hydrogen; or halogen;A is ##STR2## or O--R.sup.4 ; R.sup.3 is hydroxy; (C.sub.1 -C.sub.8)-alkoxy; (C.sub.1 -C.sub.4)-alkoxy-(C.sub.1 -C.sub.4)-alkoxy-(C.sub.1 -C.sub.4)-akoxy; (C.sub.1 -C.sub.4)-alkylthio-(C.sub.1 -C.sub.4)-alkoxy; mono- or di(C.sub.1 -C.sub.4)-alkylamino-(C.sub.1 -C.sub.4)-alkoxy; (C.sub.1 -C.sub.8)-cyanoalkoxy; (C.sub.3 -C.sub.8)-alkenyloxy; (C.sub.3 -C.sub.8)-haloalkenyloxy; (C.sub.3 -C.sub.8)-alkynyloxy; (C.sub.3 -C.sub.7)-cycloalkoxy; (C.sub.3 -C.sub.7)-cycloalkyl-(C.sub.1 -C.sub.4)-alkoxy; halo(C.sub.3 -C.sub.

Abstract: A compound of the formula ##STR1## wherein R.sub.1 is a hydrogen atom or a methoxy group, and A is a C.sub.1 -C.sub.4 alkylene group, or a pharmaceutically acceptable salt thereof. This compound is useful as a medicine, particularly as a lipoxygenase inhibitor for polyunsaturated fatty acids.

Abstract: 2-Substituted-1-naphthols are 5-lipoxygenase inhibitors which make them useful in the treatment of inflammation, obstructive lung disease and/or psoriasis. Useful 2-substituent groups are alkyls, alkenyls, alkynyls, cycloalkyls, cycloalkenyls, the groups CH.sub.2 --C.tbd.C--(CH.sub.2).sub.m R.sup.5 and CH.dbd.CH--(CH.sub.2).sub.n R.sup.5 (where m is 1-4, n is 0-3 and R.sup.5 includes phenyl, COOR.sup.9, where R.sup.9 is H or alkyl or 1-4 carbons, AR.sup.6 (where A is a methylene chain and R.sup.6 is a variety of groups including Cl, Br, I, CHO, CN, COOR.sup.9, NH.sub.2, SC(NH)NH.sub.2, phenyl, P(O)(OR.sup.9).sub.2, etc.), and CHR.sup.7 R.sup.21 (where R.sup.7 is a variety of aromatic and heterocyclic groups and R.sup.21 is H, optionally substituted phenyl and a variety of heterocyclic groups).

Abstract: Novel 1,2-cyclohexylaminoaryl amides useful as analgesic agents having very high kappa-opioid affinity and selectivity and potency and useful as analgesics, diuretics, antiinflammatory and psychotherapeutic agents are disclosed. Methods for making the compounds and pharmaceutical compositions containing them are also disclosed.