Abstract: 7-(Diphenylmethyl)oxy-9a-methoxymitosane is a novel intermediate for conversion into 7-amino and 7-oxy-9a-methoxymitosanes and is also useful for inhibiting mammalian tumor growth. The compound is prepared by reacting 7-hydroxy-9a-methoxymitosane with diazodiphenylmethane. In a preferred reaction, the compound is prepared from mitomycin C via 7-hydroxy-9a-methoxymitosane without drying (water removal). The intermediate is advantageously converted to the very effective anti-tumor agent 7-[2-(4-nitrophenyldithio) ethylamino]-9a-methoxymitosane in unexpectedly high yields using a two step process where the first step constitutes conversion to 7-[2-(2-pyridyldithio) ethylamino]-9a-methoxymitosane. or 7-[2-(3-nitro-2-pyridyldithio)ethylamino]-9a-methoxymitosane.

Abstract: Alpha-aminonitriles can be synthesized by the reaction, at ambient temperature without use of catalyst, of essentially stoichiometric amounts of amine, aldehyde (either monoaldehyde or dialdehyde) and trimethylsilyl cyanide.

Abstract: Novel compounds of the formula I ##STR1## in which X is an anion, and a process for the preparation thereof, are described. Compounds of the formula I are used as coupling reagents in peptide synthesis.

Abstract: New proline derivatives of the general formula: ##STR1## wherein R stands for a lower alkyl group and X for a N-terminal protective group conventional in amino acid chemistry or an acyl group derived from an amino acid with a protective group at the N-terminal. They have inhibitory activity against prolylendopeptidase and are relatively chemically stable as compared with known compounds of this type.

Abstract: A method is provided for deterring ethanol ingestion by a human, comprising administering to said human an amount of a compound of the formula (R.sup.1) R.sup.2)NC(X)S(O)R.sup.3 effective to cause the disulfiram-ethanol reaction in said human, wherein R.sup.1, R.sup.2 and R.sup.3 are each (C.sub.1 -C.sub.4) alkyl groups, e.g., methyl, ethyl, propyl, isopropyl, butyl, i-butyl and t-butyl.

Abstract: An improved process for the preparation of trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where 1,6-heptadien-4-ol is converted in eight operations to the desired products, as well as an improved process for the preparation of (2R-trans) and trans-(.+-.)-5-(4-fluoro-phenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetr ahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide by a novel synthesis where 4-methyl-3-oxo-N-phenylpentanamide is converted in eight operations to the desired product or alternatively 4-fluoro-.alpha.-[2-methyl-1-oxopropyl]-.gamma.-oxo-N,.beta.-diphenylbenze nebutaneamide is converted in one step to the desired product, and additionally, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahy dro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide from (R)-4-cyano-3-[[(1,1-dimethylethyl)dimethylsilyl]oxy]butanoic acid, as well as other valuable intermediates used in the processes.

Abstract: N-amino hexahydrocyclopenta imidazole-2(1H)-one derivatives useful for treating or preventing thrombo-embolic disorders and ocular diseases characterized by increased ocular pressure.

Abstract: A composition comprising(a) a 3-isothiazolone compound of the formula ##STR1## wherein R and R.sup.1 are independently selected from hydrogen, halogen or R is a (C.sub.1 -C.sub.4) alkyl group and R.sup.1 is a halogen or R and R.sup.1 may be joined to form an unsaturated 5- or 6-membered carbocyclic ring; Y is hydrogen, a (C.sub.1 -C.sub.18) alkyl group, an unsubstituted or halo-substituted alkenyl or alkynyl of 2 to 8 carbon atoms, a cycloalkyl or substituted cycloalkyl of 3 to 12 carbon atoms, an aralkyl or halo-, (C.sub.1 -C.sub.4) alkyl-, or (C.sub.1 -C.sub.4) alkoxy-substituted aralkyl of up to 10 carbon atoms, or an aryl or halo-, (C.sub.1 -C.sub.4) alkyl-, or (C.sub.1 -C.sub.4) alkoxy-substituted aryl group of up to 10 carbon atoms; and(b) an amount of a metal bromate salt sufficient to stabilize said composition;wherein said composition if free of metal nitrate salt is disclosed. Methods of use of the above compositions are also disclosed.

Abstract: The present invention relates to novel NMDA receptor antagonists and methods for their use. The present invention also provided pharmaceutical compositions comprising such NMDA receptor antagonists.

Abstract: The invention is directed to processes for the preparation of dimethyl-1,4-dihydro-2,6-dimethyl-4-(2'-nitrophenyl)-pyridine-3,5-dicarbox ylate by reacting 1-methoxy-1-(2'-nitrophenyl)-N-(2'-nitrophenyl)methylene methanamie or 1-(2'-nitrophenyl)-N,N'-bis-(2'-nitrophenyl) methylene methanediamine with methyl acetoacetate in the presence of an amine compound or by reacting the monomeric or trimeric from of 2-nitrobenzaldimine with methyl acetoacetate.

Abstract: Glycidyl azide polymer is a hydroxy-terminated aliphatic polyether containing alkyl azide groups. Such a polymer could be used as a plasticizer in composite explosives, gun and rocket propellants. However, the hydroxyl groups of the polymer react with the isocyanate of the curing agent, thereby eliminating any possible plasticizing effect. This problem is overcome by producing a diazido-terminated glycidyl azide polymer without terminal hydroxyl groups. This useful polymer is produced by reacting polyepichlorohydrin with p-toluenesulfonyl chloride in pyridine, and reacting the resulting tosylated polyepichlorohydrin with sodium azide in dimethylformamide.

Abstract: Novel herbicidal compounds of the general formula ##STR1## in which X represents a phenyl group substituted in the 2-position and optionally substituted in one or more of the 3-, 4-, 5- and 6-positions, the 2-substituent being a cyano group, or a group of the general formula CQNR.sup.1 R.sup.2 or COQR.sup.3 where Q represents an oxygen or sulphur atom and each of R.sup.1, R.sup.2 and R.sup.3 represents a hydrogen atom or an optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl, phenyl or phenalkyl group, or R.sup.1 and R.sup.2 jointly represent a hydrocarbon chain;Y represents an optionally substituted phenyl group; L represents an oxygen or sulphur atom; andZ represents a hydrogen atom or an optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl, phenyl or phenalkyl group;and salts of such compounds.

Abstract: The invention relates to new alkadienenitriles of the formula ##STR1## in which n is an integer from 5 to 9, a process for their preparation and their outstanding suitability as odororiferous substances.

Abstract: Normally liquid final Mannich condensates prepared by reacting a para C.sub.1 -C.sub.15 alkyl phenol with formaldehyde and a first polyoxyalkylene diamine to form an intermediate Mannich condensate that is reacted with formaldehyde and a second polyoxyalkylene diamine to form a final Mannich condensate, the first and second polyoxyalkylene diamines having the formula: ##STR1## wherein R represents hydrogen or methyl and R' represents an alkyl group containing 1 to 4 carbon atoms or cyanoethyl group, and n represents positive numbers having a value of 1 to about 6, the final Mannich condensate having the formula: ##STR2## wherein X and Y are polyoxyalkylene amine groups derived from the first and second polyoxyalkylene diamines and formaldehyde.

Abstract: The invention relates to novel 3-chloromethylsulfonylmethyl-4-sulfomethyl-pyrrolidinium betaines (chloromethylsulfonyl-sulfobetaines) of the general formula I and to processes for the preparation thereof. The compounds according to the formula I can be used as organic intermediates for further syntheses or, if they contain a long-chain alkyl radical, as polyfunctional surfactants. Molar quantities of diallylammonium chloride are reacted with dichloroacetic acid and twice the molar quantity of sodium hydrogen sulfite in the presence of a catalytic quantity of a peroxodisulfate and, after the addition of a catalytic quantity of iodide, the reaction solution obtained is converted by heating to 3-chloro-methylsulfonylmethyl-4-sulfomethyl-pyrrolidinium betaines (chloromethylsulfonyl-sulfobetaines) of the general formula I.

Abstract: Polymers are produced from 4 and 5 member cyclic ethers, which polymers have hydroxyl functionalities of 4.

Abstract: Cyclohexenone compounds of the formula I ##STR1## where the substituents have the following meanings: R.sup.1 substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or benzyl;A oxygen N--OR.sup.2, NR.sup.3 ;R.sup.2 substituted or unsubstituted alkyl, alkenyl, alkynyl;R.sup.3 hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, substituted or unsubstituted phenyl or benzyl;processes for their manufacture and their use for combating unwanted plant growth and for regulating plant growth.

Abstract: A compound of the formula ##STR1## wherein X has the formula --CR.sup.5 .dbd.CR.sup.6 --, --C.tbd.C-- or ##STR2## wherein ring A is phenyl, naphthyl or heterocyclic; wherein R.sup.1 is hydrogen, alkyl, alkanoyl or aroyl;wherein R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each is an electron withdrawing substituent or each is hydrogen or alkyl, alkoxy or dialkylamino, provided that when ring A is phenyl or naphthyl at least one of R.sup.2, R.sup.3 and R.sup.4 is an electron-withdrawing substituent;wherein R.sup.5 and R.sup.6, each is hydrogen, halogeno or alkylwherein R.sup.7 is alkyl or halogenoalkyl; and wherein R.sup.8 has the formula --Y--Q--R.sup.9 wherein Y is straight- or branched-chain alkylene or alkenylene; wherein Q is --O--, --S--, --SO-- or --SO.sub.2 --;and wherein R.sup.9 is alkyl of up to 6 carbon atoms which contains one or more defined substituents, processes for their manufacture and pharmaceutical compositions containing them.

Abstract: Novel pyrrolecarboxylic acid derivatives represented by the following formula: ##STR1## where R.sup.1 is a hydrogen atom, an alkyl group of 5 to 25 carbon atoms or an alkenyl group of 5 to 25 carbon atoms, R.sup.2 is a hydrogen atom, a phenyl group or an optionally substituted alkyl group of 1 to 10 carbon atoms, and R.sup.3 is a hydrogen atom, an alkyl group of 5 to 25 carbon atoms or an alkenyl group of 5 to 25 carbon atoms, or pharmaceutically acceptable salts thereof are provided.The compounds are highly effective in reducing the level of triglyceride or cholesterol in serum, and useful as an active ingredient of a pharmaceutical composition for treating hyperlipemia and arteriosclerosis.

Abstract: A process for producing glycinonitrile under substantially adiabatic reaction conditions by reacting in a tubular reactor hydrogen cyanide, formaldehyde and ammonia. The excess ammonia is flashed off and the remaining solution volatiles are evaporated and condensed to product. The resulting glycinonitrile can be saponified to the alkali metal glycinate, from which glycine can be prepared.