Abstract: Geminal dinitro compounds are prepared by reacting an organic nitro compound having a replaceable hydrogen on the carbon to which the nitro group is attached with a source of nitrite ions in the presence of an oxidizing agent and a catalytic amount of an alkali metal ferricyanide.

Abstract: Novel homocysteine thiolactone bifunctional chelating agents useful for chelating radionuclides to produce a radiodiagnostic agent for use in in vivo imaging and a method for producing this chelating agent.

Abstract: This invention relates to a novel class of heterocyclic amidinourea and heterocyclic amidinothiourea compounds wherein the heterocyclic substitution is at the 1-N urea nitrogen atom. These compounds exhibit pharmaceutical activity and may be incorporated into pharmaceutical preparations for producing anti-ulcerogenic, antisecretory, antispasmodic, antimotility, cardiovascular, antidiarrheal or antiparasitic action.

Abstract: Compounds of the formula ##STR1## in which Ar is 2-alkyl-, -alkoxy- or -halo-methyl-phenyl or .alpha.-naphthyl, each of which is further substituted,R.sub.1 is 2-furyl, 2-tetrahydrofuryl, alkenyl, cyclopropyl, .beta.-alkoxyethyl, hydroxymethyl, triazolylmethyl, imidazolylmethyl, pyrazolylmethyl, alkylsulfinyl, alkylsulfonyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, alkylsulfinyloxy, dialkylaminosulfinyloxy, phosphoric or thiophosphoric esters or amides, or alkylcarbonyloxy, andR.sub.9 is hydrogen or methyl,are microbicidally, in particular fungicidally active. The preferred compounds are those in which Ar is 2-methylphenyl, 2-methoxyphenyl, 2-chlorophenyl or .alpha.-naphthyl, each of which is further substituted by azido, and R.sub.9 is hydrogen.

Abstract: The invention provides novel N-acylamino thiophene derivatives, e.g. N-(methoxyacetyl)-N-(5-bromo-4-methyl-2-methylthiothien-3-yl)alanine methyl ester, which are useful as fungicides. Other objects of the invention are fungicidal compositions comprising such novel compounds and methods of combatting phytopathogenic fungi with the acid of said novel compounds.

Abstract: A process for resolving a racemic modification of .beta.-adrenergic aryl- or hetaryl-oxypropanolamines such as (.+-.)-2-[2-hydroxy-3-[[2-(1H-indol-3-yl)-1,1-dimethylethyl]amino]propoxy] benzonitrile into its individual enantiomers is described. The process comprises converting the racemic modification into a pair of diastereomeric urea derivatives by reaction with a chiral aralkylisocyanate; separation into the individual diastereomers; and facile regeneration of the starting amine by cleavage of the intermediate urea compound using hydrazine. This final step is improved by the addition of an .alpha.-keto carboxylic acid, such as pyruvic acid, which functions as a scavenger of nucleophilic by-products.

Abstract: The invention relates to new nitrothiophenes of the general formula ##STR1## wherein R is an alkyl group having 1 to 12 carbon atoms, which alkyl group may be substituted with a phenyl group substituted, if desired, with nitro, halogen, alkyl with 1 to 4 carbon atoms or alkoxy with 1 to 4 carbon atoms, with an alkoxycarbonyl group having 2 to 5 carbon atoms, or with a thiocyanato group, orR is a phenyl group, a pyridyl group or an N-oxypyridyl group, which groups may be substituted with nitro, halogen, alkyl with 1 to 4 carbon atoms, or alkoxy with 1 to 4 carbon atoms;R.sub.1 is a hydrogen atom, a halogen atom, an alkyl group having 1 to 4 carbon atoms, or a phenyl group substituted or not substituted with nitro, halogen, alkyl with 1 to 4 carbon atoms, or alkoxy with 1 to 4 carbon atoms;R.sub.2 is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, a cyano group, an alkanoyl group having 1 to 5 carbon atoms, an .alpha.,.alpha.-dialkoxyalkyl- or .alpha.,.alpha.

Abstract: Compounds of the formula ##STR1## in which Ar is 2-alkyl-, -alkoxy- or -halo-methyl-phenyl or .alpha.-naphthyl, each of which is further substituted,R.sub.1 is 2-furyl, 2-tetrahydrofuryl, alkenyl, cyclopropyl, .beta.-alkoxyethyl, hydroxymethyl, triazolylmethyl, imidazolylmethyl, pyrazolylmethyl, alkylsulfinyl, alkylsulfonyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, alkylsulfinyloxy, dialkylaminosulfinyloxy, phosphoric or thiophosphoric esters or amides, or alkylcarbonyloxy,R.sub.7 is hydrogen or optionally-substituted methyl or ethyl, andR.sub.8 is alkyl optionally substituted by alkoxy,are microbicidally, in particular fungicidally, active. Preferred compounds are those in which Ar is 2-methylphenyl, 2-methoxyphenyl, 2-chlorophenyl or .alpha.-naphthyl, each of which is further substituted by azido, and each of R.sub.7 and R.sub.8 is methyl.

Abstract: 3-(N-acyl-N-arylamino) and 3-(N-thionoacyl-N-arylamino)-gamma-butyrolactones and thiobutyrolactones have fungicidal activity.

Abstract: Sulfides prepared by reacting a sulfoxide with a hydrazine or hydroxylamine derivative or a quaternary salt thereof are useful starting materials for the preparation of drugs, pesticides and dyes.

Abstract: Novel homocysteine thiolactone bifunctional chelating agents useful for chelating radionuclides to produce a radiodiagnostic agent for use in in vivo imaging and a method for producing this chelating agent.

Abstract: Bis(carboxamide) derivatives being useful as histamine H.sub.2 receptor antagonists or anti-peptic ulcer agents are provided from certain dicarboxylic acid derivatives.

Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is H or alkyl; R.sup.2 and R.sup.3 are independently H, alkyl, aryl or substituted aryl; R.sup.4 is H or alkoxycarbonyl; R.sup.5 is H, acyl or a cation; and Z is thienyl or substituted thienyl.The compounds exhibit grass herbicide activity and are prepared via the reaction of the appropriately substituted cyclohexane-1,3-dione with the appropriate thienylmethoxyamine derivative and optionally acylating this product at the 3-hydroxy position or converting it to the cation salt.

Abstract: The novel compounds of the formula I are useful selective herbicides for postemergence application in crops of cereals, maize and rice.In formula I, ##STR1## A is an unsubstituted or substituted amino group, Q is a C.sub.2 -C.sub.6 alkylene bridge, Y is an oxygen or sulfur atom or an unsubstituted or substituted nitrogen atom, and Z is an unsubstituted or substituted phenyl, naphthyl or heterocyclic radical, which phenyl radical, containing the bridge member Y, can additionally carry one to four further substituents.

Abstract: The present invention relates to [(2-oxo-3-tetrahydrothienylcarbamoyl)-alkylthio]-acetic acids, their salts and esters of formula: ##STR1## in which n is 0 or 1, one of the substituents R.sub.1 and R.sub.2 is a hydrogen atom or a methyl group and the other represents a group -S-CH.sub.2 -COOR.sub.3, where R.sub.3 is a hydrogen atom or an alkali metal or a lower alkyl group or a group: ##STR2## It also relates to a process for preparing said acids, salts and esters, and to the drugs containing same.

Abstract: 3-(N-acyl-N-arylamino) and 3-(N-thionoacyl-N-arylamino)-gamma-butyrolactones and thiobutyrolactones have fungicidal activity.

Abstract: This invention covers thiophenesulfonylureas of Formula I, agriculturally suitable compositions containing them, and their method-of-use as general and/or selective preemergent and/or postemergent herbicides or plant growth regulants.

Abstract: N-Maleyl homocysteine thiolactone amide, N-maleamide homocysteine thiolactone amide, oxalyl homocysteine thiolactone hydroperchlorate, and rhodium trichloride oxalyl homocysteine thiolactone hydroperchlorate are useful as anti-neoplastic agents.

Abstract: A process for the preparation of 3-(arylamino)-tetrahydrothiophen-2-one derivatives is described in which the corresponding 3-(N-arylamino)-tetrahydrofuran-2-one derivatives are reacted with salts of thiocarboxylic acids. 3-(N-Arylamino)-tetrahydrothiophen-2-one derivatives are usable fungicides for plants.

Abstract: Antihistamines of the formula ##STR1## wherein ##STR2## is a 5 or 6 membered ring which is phenyl or heterocyclic; ##STR3## is a six membered ring which is 2,3 or 4 pyridyl or is phenyl or substituted phenyl, with the proviso that is ##STR4## is a nitrogen containing ring, ##STR5## must be phenyl; Z is an alkylene chain having 0 to 2 carbon atoms in the chain, said 2 carbon chain optionally having one double bond, said chain optionally having either a carbonyl oxygen, or a hydroxy group as a substituent; W is ##STR6## wherein p is 1 or 2 and n is 1 or 2, R.sup.1 is C.sub.1 to C.sub.6 alkyl, R.sup.2 is hydrogen or C.sub.1 to C.sub.6 alkyl, and the dotted line represents an optical double bond, R.sup.2 being absent if the double bond is present, and Y is substituted carboxylate or substituted sulfonyl. Said antihistamines have little or no sedative effects.

Abstract: Biological activity is retained while reducing toxicity to animals, particularly mammals, e.g. humans, when a physiologically-active and pharmacologically-acceptable compound (having or structurally modified to have an aldehyde function) is condensed with any of the six (mono)amino(mono)oxotetrahydrothiophenes, e.g. homocysteine thiolactone, to form a Schiff Base (a 4-butyrothiolactone-2-imine or .gamma.-thiobutyrolactone-.alpha.-imine). The invention is directed to every Schiff Base which is a condensate of a physiologically-active and pharmacologically-acceptable compound with a (mono)amino(mono)oxotetrahydrothiophene. These Schiff Bases have a unifying common property in reduced toxicity, while maintaining the biological properties "carried" by the imine substituents. They concurrently have at most an insignificant adverse affect on pharmacological activity.

Abstract: Novel carbamates derived from substituted cyclic .beta.-keto-alcohols, their preparation, and pharmaceutical formulations which contain these compounds and which may be used as hypnotics in the treatment of sleep disturbance and as sedatives.

Abstract: A novel process for making 3-(N-arylamino)-gamma-butyrothiolactones from their corresponding butyrolactone analogs is disclosed. The thiolactone products are useful intermediates for making fungicidal compounds.

Abstract: 3-(N-arylamino)-gamma-butyrolactones, butyrolactams and thiobutyrolactones are intermediates for compounds having fungicidal activity.

Abstract: A method of preparing substituted acylbenzenes is disclosed. The method comprises reacting selected acylhalides or equivalents with a selected poly-substituted benzene in the presence of an acylating catalyst comprising a clay.

Abstract: Novel hybrid 1,3-dione-carbamate compounds which exhibit utility as insecticides and acaricides. Also included are insecticidal and acaricidal compositions containing these compounds and a method of controlling insects and acarids.

Abstract: Heterocyclic sulfenamides, such as N-[2-chloro-5-(trifluoromethyl)phenyl]-N-[2,4-dinitro-6-trifluoromethyl)ph enyl]-3-nitro-2-pyridinesulfenamide, are useful as miticides, insecticides, fungicides and ovicides.

Abstract: There are described acylaniline derivatives which in the phenyl ring are substituted in the meta-position with respect to the amino group by an aliphatic oxymethyl group or aryloxymethyl group, or by an aliphatic thiomethyl group or arylthiomethyl group. Compounds of this type have a very favorable microbicidal spectrum. They are used principally for combating phytopathogenic fungi and bacteria.

Abstract: The invention concerns novel pesticidal esters of the pyrethrin or pyrethroid type in which the methylene group bonded to the ester carbonyl and/or ester oxygen bears a fluorine substituent. The compounds of the invention are active against insect pests including flies, moths, aphids and beetles and acarina pests including ticks.

Abstract: Novel N-haloacetylphenylamino carbonyl oximes represented by the formula ##STR1## wherein Ar is phenyl or substituted phenyl; R.sup.1 is halomethyl; R.sup.2 and R.sup.3 are each independently hydrogen, alkyl, phenyl, benzyl, substituted phenyl or benzyl, haloalkyl, cyanoalkyl, alkoxyalkyl, alkylthioalkyl or thiocyanoalkyl; R.sup.4 is hydrogen or alkyl; n is 0 or 1; m is 0 or 1; R is hydrogen, alkyl, alkenyl, alkynyl, alkylthioalkyl, haloalkyl, alkoxyalkyl, cyanoalkyl, phenyl, benzyl, substituted phenyl or benzyl, or R is acyl of the formula ##STR2## wherein R.sup.5 is hydrogen, alkyl, haloalkyl, alkoxyalkyl, alkylthioalkyl, alkoxy, alkylthio, acetonyl, or the group -NR'R" wherein R' and R" are independently hydrogen, alkyl or phenyl; with the proviso that R.sup.2 and R.sup.3 may be joined together to form a carbocyclic ring or a heterocyclic ring; or R and R.sup.2 may be joined together to form a heterocyclic ring; or R and R.sup.3 may be joined together to form a heterocyclic ring.

Abstract: Homocysteine thiolactone perchlorate is prepared from the corresponding homocysteine thiolactone hydrochloride and optimally about two equivalents of perchloric acid as reactants. A preferred solvent utilized is chloroform-methanol (4:1) solution and a preferred temperature range is 0.degree.-85.degree. C. with the lower limit dependent upon the particular solvent and the upper limit of about 186.degree. C. dependent upon the melting point of the product crystals. The preferred perchloric acid reactant may be replaced with perchlorate salts such as AgClO.sub.4 or KClO.sub.4. The product perchlorate salt is soluble in organic solvents, whereas other known salts such as the hydrochloride are only water soluble. This property is thought to influence the growth effect of the perchlorate salt in animals, such as rabbits, and to influence the unique effect of the perchlorate salt on the growth of malignant tumors in animals, such as mice.

Abstract: 3-(N-acyl-N-arylamino)-gamma-butyrolactones and thiobutyrolactones have fungicidal activity.

Abstract: Novel 9-substituted or unsubstituted thienyl-3,7-dimethyl-nona-2,4,6,8-tetraene derivatives, useful as antitumor agents as well as processes for their preparation and novel intermediates are disclosed.

Abstract: A process for making a compound of the formula ##STR1## which process comprises contacting, in the absence of an acid acceptor, an acyl halide with an aniline substituted gamma-butyrolactone in the presence of a non-basic solvent and at a temperature between 65.degree. and 150.degree. C. Thus, 3-(N-chloroacetyl-N-2,6-dimethylphenylamino)-gamma-butyrolactone is prepared by a process comprising contacting, in the absence of an added acid acceptor, chloroacetylchloride with 3-(N-2,6-dimethylphenylamino)-gamma-butyrolactone in the presence of a non-basic organic solvent and at a temperature between 65.degree. and 150.degree. C. Preferably, the 3-(N-2,6-dimethylphenylamino)-gamma-butyrolactone is formed by reacting alpha-bromo-gamma-butyrolactone with dimethylaniline in the presence of water and in a non-basic organic solvent, and the 3-(N-2,6-dimethylphenylamino)-gamma-butyrolactone in the organic solvent is phase separated and fed straight through to the acetylation step.

Abstract: A process for producing a lactone-substituted aniline wherein a 3-halo-tetrahydro-2-oxofuran is reacted with an aniline in the presence of water and a base at a temperature between 80.degree. and 160.degree. C. and wherein the base is added at a sufficiently slow rate so that the pH does not exceed about 7.5.

Abstract: Novel N-haloacetylphenylamino carbonyl oximes represented by the formula ##STR1## wherein Ar is aryl, R.sup.1 is halomethyl, R.sup.2 is hydrogen, alkyl or aryl, R.sup.3 is hydrogen, alkyl or aryl, n is 0 or 1 and R is hydrogen, aryl, alkyl, alkenyl or alkynyl, with the proviso that R.sup.2 and R.sup.3 may be joined together to form a carbocyclic ring of 5 to 6 carbon atoms or a heterocyclic ring of one N, O or S hetero atom and 4 to 5 carbon atoms. The oxime compounds are useful as herbicides and plant growth regulators.

Abstract: A process for producing a lactone-substituted aniline wherein an alpha-halo-gamma-butyrolactone is reacted with an aniline in the presence of water at a temperature between 80.degree. and 160.degree. C. Thus, 3-(N-2,6-dimethylphenylamino)-gamma-butyrolactone is prepared by reacting an alpha-halo-gamma-butyrolactone with 2,6-dimethylaniline in the presence of water and an inert organic solvent at a temperature between 80.degree. and 160.degree. C. This process is advantageously combined with a subsequent acylation step to provide a continuous means for making materials such as 3-(N-chloroacetyl-N-2,6-dimethylphenylamino)-gamma-butyrolactone.