Abstract: Process for preparing carboxylic acids by converting a glycidonitrile to a 2-oxopropionitrile via use of an ionic Lewis acid, and conversion of the 2-oxopropionitrile to the carboxylate salt with a base and of the salt to the carboxylic acid with acid.The process is especially useful for the preparation of 2-(p-isobutylphenyl)propionic acid, (lbuprofen), also known as Motrin, a known and highly active antiinflammatory agent as well as a host of other carboxylic acids which are known in the art as useful compounds.

Abstract: 3-Substituted 4-(.alpha.-amino-.alpha.-phenyl-o-tolyl)-4H-1,2,4-triazoles, 2-substituted 1-(.alpha.amino-.alpha.-phenyl-o-tolyl)imidazoles, pharmacologically acceptable acid addition salts thereof and processes for their production. The compounds of this invention and the pharmacologically acceptable acid addition salts thereof are useful as sedatives, hypnotics, anticonvulsants, tranquilizers, and muscle relaxants. They are also useful as feed additives for increasing growth rate and feed efficiency of livestock and poultry.

Abstract: This invention relates to novel benzospiran derivatives embraced by the formula ##STR1## wherein the sum of A and B is at least the integer 2; A is selected from the group consisting of --(CH.sub.2).sub.n wherein n is 1 through 5 and --(CH.sub.n H.sub.2n --.sub.2 XY)-- wherein X is selected from the group consisting of hydroxy, acetoxy, amino and acetamido and Y is hydrogen, and X when taken together with Y is selected from the group consisting of =O and =CR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are selected from the group consisting of hydrogen and lower alkyl of 1 through 3 carbon atoms; B is absent or --(CH.sub.2).sub.n wherein n is 1 through 3; R.sup.1 is selected from the group consisting of hydrogen and lower alkyl of 1 through 3 carbon atoms; R.sup.

Abstract: Preparing 2-(substituted phenyl)propionic acids by heating a mixture containing succinic acid anhydride with a 2-(2-oxo-3-cyclohexenyl)propionic acid derivative and then recovering the 2-(2-substituted phenyl)propionic acid derivative from the reaction mixture. The heated mixture can also contain other acids such as an 2-(1-carboxy-2-oxo-3-cyclohexenyl)propionic acid.

Abstract: Chiral, hinged and functionalized host multiheteromacrocycles of the oxygen, nitrogen and sulfur-containing type are disclosed possessing holes sized to afford selective complexation of specific guest substances and shapes to recognize chirally guest molecules by virtue of the chiral steric barrier of the 2,2'-diheteroatom-1,1'-binaphthyl grouping, the naphthyl-naphthyl dihedral angle, and the provision of ortho positioned side chain substituents (arms) bearing terminal functional groups which act as counterions or additional complexing sites, and the provision of remote position side chain substituents used to control solubility and volatility properties or to bond the multiheteromacrocycles to solid supports.

Abstract: Pharmaceutical compositions comprising, in unit dosage form, from about 0.5 mg. to about 100 mg. of a compound of the formula ##SPC1##Wherein R and R' are hydrogen, methyl or ethyl, R.sub.1 is hydrogen or lower alkyl of 1 through 3 carbon atoms, R.sub.2 is hydrogen, lower alkyl of 1 through 3 carbon atoms, fluorine, chlorine, bromine, nitro, trifluoromethyl or lower alkylthio of 1 through 3 carbon atoms, and the pharmacologically acceptable acid addition salts thereof, in association with a pharmaceutical carrier. The process is the administration of the above compositions to humans or animals at a dose of from about 0.01 mg./kg./day to about 2 mg./kg./day for anti-anxiety or anti-depressant effects.

Abstract: This invention relates to new and novel processes for the production of carboxylic acids from glycidonitriles in high yields and high purity. The processes are especially useful for the preparation of 2-(p-isobutylphenyl)propionic acid, (lbuprofen), also known as Motrin, a known and highly active antiinflammatory agent as well as a host of other carboxylic acids which are known in the art as useful compounds.

Abstract: Preparing 1-halo-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines by reacting an N-halosuccinimide with a 2-[3-(phthalimidomethyl)triazolyl]benzophenone to form the 2-[5-halo-3-(phthalimidomethyl)triazolyl] benzophenone and reacting the 2-[5-halo-3-(phthalimidomethyl)triazol-4-yl]benzophenone with hydrazine or a primary amine in an organic liquid solvent medium at 25.degree. to 100.degree. C. The products of the process have CNS tranquilizer and sedative properties but are also of interest for use as intermediates to prepare 2,4-dihydro-6-phenyl-1H-s-triazolo[4,3-a] [1,4]benzodiazepin-1-ones which are of clinical interest for their CNS tranquilizer, sedative and anti-depressant drug use properties in mammalian animals including humans.

Abstract: Process for preparing carboxylic acids by (1) reacting a glycidonitrile with a carboxylic acid halide in the presence of a catalytic amount of a tertiary amine or acid salt thereof to form a 2-acyloxy-3-halo-propionitrile, (2) dehydrohalogenating the halogenated acylate from step (1) to form the acyloxy acrylonitrile intermediate (enol-acylate) (3) hydrolyzing the enol-acylate from step (2) with aqueous base to form the carboxylic acid salt, and (4) acidifying the carboxylic acid salt with acid to form the carboxylic acid. Salts of persulfate and hypochlorite ions can be added to destroy cyanide ion. The process can be used to prepare a wide variety of carboxylic acids, e.g., 2-(4'-isobutylphenyl)propionic acid, now known generally as ibuprofen, a highly active anti-inflammatory drug.

Abstract: Process for preparing carboxylic acids by converting a glycidonitrile to the enol acylate via hydrohalogenation, acylation and dehydrohalogenation procedures, and conversion of the enol acylate to the carboxylate salt with a base and of the salt to the carboxylic acid with acid. Cyanide content in the mixture is destroyed by adding persulfate or hypochlorite salts. This process, can be used, e.g., to prepare 2-(4'-isobutylphenyl)propionic acid, now known generically as ibuprofen, a highly active anti-inflammatory drug, as well as a host of other useful carboxylic acids.

Abstract: 3-Substituted-4-(.alpha.-amino-.alpha.-phenyl-o-tolyl)-4H-1,2,4-triazoles 2-substituted 1-(.alpha.-amino-.alpha.-phenyl-o-tolyl)imidazoles, pharmacologically acceptable acid addition salts thereof and processes for their production. The compounds of this invention and the pharmacologically acceptable acid addition salts thereof are useful as sedatives, hypnotics, anticonvulsants, tranquilizers, and muscle relaxants. They are also useful as feed additives for increasing growth rate and feed efficiency of livestock and poultry.

Abstract: Multiheteromacrocycles are disclosed that contain as part of the macrocycle, assemblies of 2,6-dimetylylpyridine (and their corresponding amine oxides), 2,5-dimethylylfuran, 2,5-dimethylyltetrahydrofuran, Diels-Alder adducts of 2,5-dimethylylfuran (and their reduction products), 2- and 4-substituted 1,3-dimethylylbenzenes, pentamethylene, or p-phenylene coupled through oxygen to one another or to ethylene, o-phenylene, or 1,1-binaphthyl-2,2- units (always coupled through oxygens) to form multidentate ligands for complexing selectively alkylammonium or metal cations.

Abstract: This invention relates to novel 4-(substituted alkoxy)-4-(substituted phenyl)cyclohexylamines embraced by the formula ##SPC1##Wherein .about. is a generic expression denoting cis and trans stereoconfiguration and mixtures thereof, with the proviso that when the stereoconfiguration of the linkage connecting the cyclohexane ring and R.sup.3 O is is cis to the amino group, the linkage connecting the cyclohexane and phenyl rings is always trans, and vice versa; R is selected from the group consisting of lower alkyl of 1 through 4 carbon atoms, chlorine, fluorine, bromine, trifluoromethyl, and lower alkoxy of 1 through 4 carbon atoms; R' has the same meaning as R and in addition hydrogen; R.sup.1 is selected from the group consisting of hydrogen and lower alkyl of 1 through 4 carbon atoms; R.sup.

Abstract: This invention relates to novel 4-phenylcyclohexylamines embraced by the formula ##SPC1##Wherein .about. is a generic expression denoting cis and trans stereoconfiguration and mixtures thereof; R is selected from the group consisting of alkyl of from one through four carbon atoms, fluorine, chlorine, bromine, trifluoromethyl, nitro and alkoxy of from one through four carbon atoms; R' and R.sup.1 are selected from the group consisting of hydrogen and alkyl of from one through four carbon atoms; R.sup.

Abstract: Novel azepine spiro indans, azepine spiro tetralins, pharmacologically acceptable acid addition salts thereof and processes for their production. The compounds of this invention and the pharmacologically acceptable acid addition salts thereof have central nervous system activity, they are especially useful as central nervous system depressants.

Abstract: Cis and trans isomers of 1,2-diphenyl-1,2,3,4-tetrahydronaphthalenes, novel processes for the preparation thereof, and novel intermediates are disclosed herein. The novel 1,2-diphenyl-1,2,3,4-tetrahydronaphthalenes have utility as antifertility estrogenic, anti-estrogenic, anti-spermatogenic, cholesterol lowering and lipid normalizing agents.

Abstract: Novel 6-substituted 4H-imidazo[1,2-a][1,4]benzodiazepines, the intermediate 5-substituted-2-(2-alkynylamino)-3H-1,4-benzodiazepines, pharmacologically acceptable acid addition salts thereof, and processes for their production. The compounds of this invention and the pharmacologically acceptable acid addition salts thereof are central nervous system depressants. They are useful as sedatives, hypnotics, tranquilizers, muscle relaxants and anticonvulsants, and also as feed additives for increasing growth rate and feed efficiency of livestock and poultry, milk production in the mammalian species and egg production in avian species.

Abstract: Process for preparing glycidonitriles in which a ketone or aldehyde is reacted with chloroacetonitrile under substantially anhydrous conditions using inorganic alkali metal bases in a solvent medium containing at least about 3 percent liquid volume of a dipolar, aprotic liquid such as dimethylformamide, any balance of solvent being a nonpolar organic liquid.

Abstract: This invention relates to novel benzospiran derivatives embraced by the formula ##SPC1##Wherein the sum of A and B is at least the integer 2; A is selected from the group consisting of --(CH.sub.2).sub.n -- wherein n is 1 through 5 and --(C.sub.n H.sub.2n --.sub.2 XY)-- wherein X is selected from the group consisting of hydroxy, acetoxy, amino and acetamido and Y is hydrogen, and X when taken together with Y is selected from the group consisting of =O and =CR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are selected from the group consisting of hydrogen and lower alkyl of 1 through 3 carbon atoms; B is absent or --(CH.sub.2).sub.n -- wherein n is 1 through 3; R.sup.1 is selected from the group consisting of hydrogen and lower alkyl of 1 through 3 carbon atoms; R.sup.