Abstract: The present invention is concerned with certain novel halogenobenzoic acid derivatives of the following formula, ##STR1## wherein R is a chlorine atom, amino group or hydroxy group, X is a chlorine atom or bromine atom, which are useful intermediates for the synthesis of antibacterial agent.

Abstract: The invention relates to several aryloxy-alkane alcohols, for example 1-(3-(1-hydroxy-1-methylhexyl) phenoxy methyl)-2-methoxy-naphthalene, 2-(1-(3-(1-hydroxy-2,2-dimethylhexyl)phenoxy)ethyl naphthalene, 1-(3-6-phenoxy-1-hydroxyhexyl)phenoxy methyl)-4-methoxy naphthalene, 2-(3-(1-hydroxyhexyl) phenoxymethyl) naphthalene and 2-(3-(1-hydroxyhexyl)phenoxymethyl)-1,2,3,4-tetrahydro naphthalene, methods for their preparation and their use for treating inflammatory and allergic conditions in a mammal.

Abstract: This invention relates to a diazonium compound of the formula: ##STR1## wherein Z is selected from the group consisting of biotin, an antigen, an antibody, a photoreactive group, a fluorescent group and heavy metal-containing compounds;X is an alkylene group containing up to 18 carbon atoms in the principle chain and a total of up to 24 carbon atoms or a substituted alkylene group containing up to 18 carbon atoms in the principle chain with substituents selected from the group consisting of solubility-enhancing groups and cleavable --S--S-- containing moieties;Ar is an unsubstituted or substituted aryl or heteroaryl; andY is an anion and n is an integer from 1-3.Such compounds are useful as components for nucleic acid probes.

Abstract: Herbicidally active thiolcarbamates are employed in combination with a certain amide extender compound, the latter in sufficient quantity to minimize soil degradation and to prolong the soil life of the former. As a result, the herbicidal effectiveness of the thiolcarbamate herbicide is significantly enhanced and prolonged, rendering a single application or multiple applications of the herbicide effective over a longer period of time. Such herbicidal compositions can optionally contain a non-phytotoxic antidotally effective amount of thiolcarbamate herbicide antidote.

Abstract: A novel polyprenyl compound such as a polyprenyl carboxylic acid amide is disclosed. It has antithrombic and antiplatelet aggregation activity.

Abstract: Synthetically produced substantially pure biologically active compounds having the general formula ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.20 alkyl, alkenyl, aryl, aralkyl, cycloalkyl, alkylcycloalkyl, cycloalkylalkyl, cycloalkenyl, alkylcycloalkenyl, or cycloalkenylalkyl;R.sub.2 is hydrogen, C.sub.1 -C.sub.10 alkyl or an amide-substituted alkyl having up to 10 carbon atoms;R.sub.3 is a cyclic, straight or branched chain hydrocarbon group having 2-12 carbon atoms, particularly --(CH.sub.2).sub.n --, wherein n is 2-12; orR.sub.2 and R.sub.3 are linked together to form an alkylene chain; andR.sub.4 is selected from ##STR2## (substituted or unsubstituted carbamimidoyl), ##STR3## (dimethylpyrimidyl), or ##STR4## (carbamyl) wherein each of R.sub.5, R.sub.6, and R.sub.7 is hydrogen or the same or different C.sub.1 -C.sub.8 alkyl group. The compounds are useful as bactericides for a wide variety of bacteria, including S.pyogenes, B.subtilis, K.pneumoniae, M.avium, B.fragilis, C.perfringens and C.albicans.

Abstract: A novel polyprenyl compound such as a polyprenyl carboxylic acid amide is disclosed. It has antithrombic and antiplatelet aggregation activity.

Abstract: A process for the perfluoroalkylation of aromatic derivatives. In a first stage, an aromatic derivative, sulfur dioxide and a metal selected from the group consisting of zinc, aluminum, manganese, cadmium, magnesium, tin, iron, nickel and cobalt, are brought into contact in a solvent, preferably a polar aprotic solvent. In a second stage, a perfluoroalkyl bromide or iodide is added to react with the aromatic derivative.

Abstract: Disclosed herein are a derivative of dihydroxybenzamide represented by the formula(I): ##STR1## wherein (1) R.sup.1 represents a hydrogen atom or a lower alkyl group and R.sup.2 represents a straight chain-alkyl group of 4 to 12 carbon atoms, a branched chain-alkyl group of 4 to 12 carbon atoms, a cyclo-alkyl group of 4 to 12 carbon atoms, ##STR2## wherein n is an integer of 1 to 6, or a pyridyl group which is substituted or unsubstituted, or (2) R.sup.1 and R.sup.2 are cyclized to make a heterocycle containing amino group represented by the formula ##STR3## wherein X represents a nitrogen atom or a methine and Y represents a hydrogen atom, an alkyl group of 1 to 6 carbon atoms or a phenyl group, and a pharmaceutical composition containing the same.

Abstract: The invention relates to new benzoylurea compounds of the general formula ##STR1## wherein R.sub.1 is a halogen atom,R.sub.2 is a hydrogen atom or a halogen atom,R.sub.3 is a hydrogen atom or represents 1 or 2 substituents which are selected from the group consisting of chlorine, methyl and trifluormethyl,R.sub.4 is a hydrogen atom or represents 1-3 substituents which are selected from the group consisting of halogen, and alkyl, alkoxy, haloalkyl and haloalkoxy, having 1-4 carbon atoms,X is N or CH,n is 0 or 1, andR.sub.5 is a hydrogen atom, an alkyl group having 1-6 carbon atoms, an alkenyl group having 2-6 carbon atoms, or a cycloalkyl group having 3-6 carbon atoms, with the proviso, that, if n is 0 and R.sub.5 is a hydrogen atom, R.sub.3 is a hydrogen atom.The compounds have an insecticidal and acaricidal activity. After having been processed to compositions, the compounds may be used for the control of insects and/or mites in a dosage of 1 to 5000 grams of active substance per hectare.

Abstract: Provided is a method for preparing diaryl iodonium salts represented by the formula:[Ar.sub.1 --I.sup..sym. --Ar.sub.2 ]HSO.sub.4.sup..crclbar.wherein Ar.sub.1 and Ar.sub.2 respectively are an aryl group which may be substituted with an electron donor group and which may be the same or different which comprises subjecting a compound represented by the formula Ar.sub.1 --H wherein Ar.sub.1 is as defined above and a compound Ar.sub.2 --I wherein Ar.sub.2 is as defined above to a coupling reaction in a sulfuric acid solution containing an oxidizing agent and diluted with a diluting agent to a concentration of 85% by weight or less at a reaction temperature in the range from -20.degree. to +35.degree. C.

Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.

Abstract: A process for the preparation of 1,4-oxazepinones and thiones having the formula: ##STR1## wherein A is an aromatic ring selected from benzene, naphthalene, quinoline or pyridine; n is 1 to 3; Z is an amino radical; R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl; and R.sup.4 and R.sup.5 are hydrogen and loweralkyl starting from chloroaromatic carboxylates and alkanolamines is disclosed.

Abstract: The pot life of a mixture of an epoxide resin and a curing agent comprising a compound containing a plurality of amine groups is improved by carbonating the curing agent.

Abstract: The present invention provides a process for the preparation of aryl carboxylic acids and derivatives thereof by the carbonylation of aryl sulfonyl chlorides. The aryl sulfonyl chlorides are reacted with carbon monoxide and water or an alcohol or amine in the presence of a zero-valent metal catalyst consisting essentially of palladium.

Abstract: 2-Haloethylamides are prepared by reaction of 2-oxazolidinone or C.sub.1-6 alkyl or phenyl derivatives thereof with an acid halide.

Abstract: The present invention provides a process for the preparation of aryl carboxylic acids and derivatives thereof by the carbonylation of triaryl sulfonium salts. The triaryl sulfonium salts are reacted with carbon monoxide and water or an alcohol or amine in the presence of a triaryl phosphine and a zero-valent metal catalyst selected from palladium or rhodium.

Abstract: Sulfonyl or carbonyl derivatives of inositols are found to be effective phospholipase C inhibitors and thereby potent anti-inflammatory and analgesic agents. These inositol derivatives are prepared by condensation of a protected inositol with a substituted sulfonic or carboxylic acid derivative followed by removal of protecting groups.

Abstract: Cis- and trans-N-[2-amino(oxy- or thia group-substituted-cycloaliphatic)]benzeneacetamide and -benzamide compounds, e.g., 3,4-dichloro-N-[4,4-dimethoxy-2-(1-pyrrolidinyl)cyclohexyl]-N-methylbenzen eacetamide, and salts thereof, are provided. These compounds have analgesic properties. Processes for their preparation are disclosed. Pharmaceutical compositions and methods of use are also provided.

Abstract: A novel ethynylation process is disclosed which provides an expanded series of novel ethylnyl-terminated aromatic compounds having base sensitive substituents and which facilitates the economic preparation of prior art ethynyl-substituted aromatic compounds.

Abstract: Cis- and trans-N-[2-amino(adjacenty substituted bis(alkyloxy), bis(alkylthio), alkylthio or mercapto group substituted)-cycloaliphatic]benzeneacetamide and -benzamide compounds, e.g., (.+-.)-(1.alpha.,2.beta.)-4-bromo-N-[3,3-dimethoxy-2-(1-pyrrolidinyl)cyclo hexyl]-N-methylbenzamide, and salts thereof, are provided. These compounds have analgesic properties. Processes for their preparation are disclosed. Pharmaceutical compositions and methods of use are also provided.

Abstract: Fluorinated diaminobutane compounds in vivo are inhibitors of gamma-aminobutyric acid transaminase and have the following formula: ##STR1## wherein: R.sub.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl, or phenyl-(C.sub.1 -C.sub.4 alkyl);R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl-(C.sub.1 -C.sub.4 alkyl), or R.sub.4, where R.sub.4 is as defined below;R.sub.3 represents hydrogen, or, except when R.sub.2 represents R.sub.4, R.sub.4, where R.sub.4 is as defined below;each R.sub.4, independently, represents C.sub.2 -C.sub.5 alkylcarbonyl, phenylcarbonyl, phenyl-(C.sub.1 -C.sub.4 alkyl) carbonyl, or an aminocarboxylic acid residue derived by removal of an hydroxy group from the carboxy moiety of an L-aminocarboxylic acid; andp represents 1 or 2,and pharmaceutically acceptable acid addition salts thereof.

Abstract: New amidine/isocyanate adducts are particularly useful as catalysts for hardening epoxy resins, in particular pulverulent coating compositions based on epoxy resins. New bicyclic amidines are excellent starting materials for manufacturing these amidine/isocyanate adducts.

Abstract: Fluorinated aminobutyric acid and diaminobutane compounds in vivo are inhibitors of gamma-aminobutyric acid transaminase and have the following formula: ##STR1## wherein: Y represents hydrogen or fluorine;Z represents --CH.sub.2 NR.sub.1 R.sub.2, where R.sub.1 and R.sub.2 are as defined below, or --COR.sub.3 where R.sub.3 is as defined below;R.sub.a represents hydrogen or R.sub.4, where R.sub.4 is as defined below;R.sub.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl or phenyl-(C.sub.1 -C.sub.4 alkyl);R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl-(C.sub.1 -C.sub.4 alkyl) or, when R.sub.a is hydrogen, R.sub.4, where R.sub.4 is as defined below;R.sub.3 represents hydroxy, or when R.sub.a is hydrogen, C.sub.1 -C.sub.8 alkoxy, --NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 are as defined below, or an aminocarboxylic acid residue derived by removal of an hydrogen atom from the amino moiety of an L-aminocarboxylic acid;each R.sub.4, independently, represents C.sub.2 -C.sub.

Abstract: A process for the preparation of a 3-bromo-4-fluorobenzaldehyde acetal of the formula ##STR1## in which R.sup.1 is methyl or ethyl,which comprises reacting a 3-bromo-4-fluoro-benzoic acid halide with ammonia to form 3-bromo-4-fluoro-benzoic acid amide, dehydrating said amide to form 3-bromo-4-fluoro-benzonitrile, reacting the nitrile with formic acid in the presence of a catalyst at a temperature between about 0.degree. and 150.degree. C. to form 3-bromo-4-fluorobenzaldehyde, and reacting said aldehyde with R.sup.1 OH or a derivative thereof capable of forming an acetal. The amide and nitrile are new compounds. The acetals are known intermediates in the synthesis of pyrethroid-like insecticides.

Abstract: A process for selective cracking of 1,4-disubstituted benzene compounds having at least one polar substituent. Mixtures containing isomers of such a compound are brought into contact with a specified type of shape selective crystalline zeolite catalyst under conditions of temperature and pressure conducive to reaction of said benzene compound, thereby selectively reacting the 1,4-disubstituted isomer in preference to the 1,2- and 1,3-disubstituted isomers of said polar benzene compound. The shape selective zeolite catalysts employed herein are crystalline zeolites characterized by a silica to alumina ratio of at least about 12 and a constraint index within the approximate range of 1 to 12.

Abstract: The present invention relates to the use of telluroxides as mild and selective oxidizing agents serving to oxidize certain functions, notably >C.dbd.S groups, in the presence of other relatively easily oxidized functions which remain unaffected; telluroxides of interest as oxidizing agents include, for example, compounds of the formula: ##STR1## wherein R and R.sup.1, which may be the same or different, each represent an optionally substituted aryl or heterocyclic group; or R and R.sup.1 together with the tellurium atom therebetween represent a heterocyclic ring, which may contain one or more further heteroatoms, and which may carry substituents and/or fused aromatic rings.

Abstract: A radioimmunoassay procedure has been discovered for bupropion [(.+-.)-2-t-butylamino-3-chloropropiophenone], an antidepressant compound, in biological fluids. Novel compounds of formula ##STR1## wherein either R.sub.2 is oxygen and R.sub.1 is (CH.sub.2).sub.n -0-(CO).sub.m -(CH.sub.2).sub.p -COOH where n is an integer from 0 to 5, m is 0 or 1, and p is an integer from 1 to 4; or R.sub.1 is hydrogen and R.sub.2 is N-O-(CH.sub.2).sub.q -COOH where q is an integer from 1 to 3, and novel methods of making them and novel intermediates useful therein are disclosed. Novel immunogens for raising bupropion specific antisera, and novel methods of making them are disclosed comprising conjugates of the novel compounds and suitable carrier material. The drug is added to the antisera together with novel radiolabeled competitor of formula ##STR2## wherein R' is a suitable radioisotope as described above and R.sub.3 is hydrogen, R.sub.4 is CL, and R.sub.5 is oxygen, orR' is hydrogen and either(a) R.sub.3 is H and R.sub.

Abstract: Novel valuable N-chloromethyl-carboxylic acid anilides, a process for their preparation, and their use for the preparation of novel valuable N-carboxylic acid anilides.

Abstract: Benzotrihalides are prepared by pyrolyzing a substituted phenyl trihaloacetate of the formula ##STR1## wherein each X is halo, nitro, alkyloxy, aryloxy, aralkyoxy, cyano, lower alkyl, haloalkyl, haloalkyloxy, alkenyl, haloalkenyl, carbamoyl, N,N-dialkylcarbamoyl, N,N-diarylcarbamoyl, or N,N-diaralkyloxy;Y is halo; andn is an integer of from 1 to 5. As an example, 4-chlorophenyl trichloroacetate is pyrolyzed at 550.degree. C. to 4-chlorobenzotrichloride.

Abstract: The process of the invention for preparing a N-(2-substituted aminoethyl)amide of the formula: ##STR1## comprises contacting one or more compounds of the formula: ##STR2## with an amine of the formula: ##STR3## wherein A is nitrogen or a quaternary nitrogen of the formula: ##STR4## wherein B is ##STR5## when A is nitrogen and B is ##STR6## when A is IV; whereinX.sup..crclbar. is a counterion;b is zero or one; andR.sub.1 -R.sub.9 are as defined in the specification.In a preferred embodiment, the process is catalyzed by a Lewis acid or a protonic acid with a non-nucleophilic counterion.

Abstract: This invention relates to a process for reducing amidine formation during reduction of organonitriles. The process comprises including a boron compound in the reaction medium in sufficient amount to complex the amidine compound as it is formed.

Abstract: Polyoxyalkylene compounds having at least four oxyalkylene units and one or two terminal hydroxyl groups are etherified by reacting same with organic primary chlorides or bromides in the presence of an aqueous, at least 30% by weight solution of sodium or potassium hydroxide to produce the corresponding etherified polyoxyalkylene derivatives. The molar ratio of the organohalide to the hydroxyl group(s) of the polyoxyalkylene compound is at least 1.2, and the molar ratio of the alkali metal hydroxide to such hydroxyl group(s) is at least 1.

Abstract: Certain radioiodine containing amides useful as brain imaging agents are disclosed. The compounds of the subject invention are represented by the formula ##STR1## wherein I is a radioisotope of iodine with I-123 being preferred, R.sub.1 and R.sub.2 are the same or different and are selected from the grooup consisting of hydrogen, hydroxy, alkyl, aryl, substituted aryl, aralkyl, anilino and carbamoylmethyl or R.sub.1 and R.sub.2 taken together with the nitrogen to which they are attached form a 5- or 6-membered ring.

Abstract: Sets of certain halogenated aromatic organic compounds, for example, N-alkyl tetrahalophthalimides, have been found useful as chemical tags when employed in a thermal particulating organic resin. Improved tagging performance has been achieved over extended use periods at temperatures up to 140.degree. C., if the tags are microencapsulated prior to incorporation into the particulating organic resin.

Abstract: Decarboxylation of carboxylic acids using diazabicycloalkenes and, if desired, also a simple copper salt, as the means for decarboxylation.

Abstract: Surfactants having an HLB of from about 12 to about 20, preferably 14 to about 20, are disclosed which correspond to formulas I and II: ##STR1## wherein: R.sub.1 is a nonpolymerizable hydrocarbyl or inertly-substituted hydrocarbyl group of at least 8 carbon atoms; R.sub.2 is hydrogen or alkyl; X is ##STR2## Y is a terminal inorganic or organic group; and n is at least 2.

Abstract: A process for preparing trifluoromethylphenyl nitro phenylethers which comprises treating a trifluoromethylhalobenzene with a base in a cosolvent system to afford a trifluoromethyl phenolate which may be isolated as its free phenol or reacted with an appropriately substituted halobenzene to afford a diphenylether herbicide or a precursor thereto.