Abstract: Anti-ulcer agents having a methylsulfinyl bridge between a substituted pyridine moiety and a substituted benzimidazole moiety are prepared by oxidizing the corresponding compounds, having a methylthio bridge, with magnesium monoperoxyphthalate in a suitable solvent. The reaction may be run in an aromatic hydrocarbon solvent, wherein the product may crystallize out of the reaction solution and may be directly isolated by filtration.

Abstract: A process for introducing a 1,2 double bond into a compound of the formula ##STR1## which comprises the process of (a) treating the compound of formula I with oxalyl chloride; (b) brominating the product of step (a) followed by in situ dehydrobromination; (c) deprotecting the product of step (b) to yield the .alpha. and .beta. isomers; (d) dehydrobrominating the product of step (c), which results in the introduction of a double bond at the 1,2 position.

Abstract: 10,11 Dihydro-11-exo-hydroxy-5-methyldibenzo[a,d]cyclohepten-5,10-imine is prepared in a four step synthesis which uses an electrochemical cyclization to form the 5,10-imine bridge in about a 50% yield.

Abstract: A novel acylation process using an alkali metal bromide and a dialkylaminopyridine to form a sterically hindered ester functionality from an alkanoyl chloride and an alcohol is disclosed.

Abstract: This invention relates to a process for preparing .beta.-lactams by electrochemically deblocking N-substituting .beta.-lactams using anodic oxidation.

Abstract: A novel synthon useful in the conversion of penicillin is a compound of the formula ##STR1## wherein R.sub.3 is a number of the group consisting of trimethyl-silyl, t-butyl dimethyl silyl, trimethyl silyl, methyl, benzyl or nitrobenzyl, and R.sub.5 is the same or different member of the group R.sub.3 is prepared by the naphthalene sulfonyl azide exchange reaction with benzyl acetoacetate, p-nitrobenzylacetoacetate, or methylacetoacetate to obtain the corresponding 2-diazo compound which is then silylated in hexamethyl-disalazine.

Abstract: A process for preparing .alpha.-alkyl amino acids by enantioretentive .alpha.-alkylation of .alpha.-amino acids is described. The products are bioactive compounds including some useful as therapeutic agents.

Abstract: A stereospecific conversion of penicillin to thienamycin, using diisopropylamine borane and magnesium trifluoroacetate to prepare the hydroxyethyl side chain and acetoacetate dianion equivalent disilylethyl to prepare the .beta.-ketoester side chain.

Abstract: Substituted-1,2,5-thiadiazole-1-oxides, their preparation and pharmaceutical use as elastase inhibitors are disclosed.

Abstract: 2-(3-Substituted amino-2-hydroxypropoxy)-3-substituted pyrazine compounds optionally having substituents in the 5 and/or 6 positions, possessing .beta.-adrenergic blocking properties are described. The products are prepared by reaction of a 2-chloro (or hydroxy) pyrazine with a 5-hydroxymethyl (or sulfonyloxymethyl) oxazolidine followed by acid hydrolysis.

Abstract: A method of preparing 2,4-difluoroaniline by reacting 2,4,5-trichloronitrobenzene with a fluorinating agent to form 2,4-difluoro-5-chloronitrobenzene which is then hydrogenated with hydrogen in the presence of a catalyst to form 2,4-difluoroaniline.

Abstract: An improved process for the preparation of thiazoles is disclosed. The process utilizes a substituted imine and sulfur dioxide heated in the presence of a catalyst. The thiazoles are known important chemical intermediates.

Abstract: An improved process for preparing the antibiotic compound 7.beta.-(2-thienylacetamido)-7-methoxy-3-carbamoyloxymethyl-3-cephem-4-car boxylic acid, from the N-blocked esters of the compound 7.beta.-(D-5-amino-5-carboxyvaleramido)-3-carbamoyloxymethyl-7-methoxy-3-c ephem-4-carboxylic acid (Cephamycin C), by conducting the transacylation of the latter in a homogenous solution containing N-trimethylsilyl loweralkyl carbamates.

Abstract: Improved method of preparing 5-(2,4-difluorophenyl)salicylic acid and derivatives which favors formation of the desired end product over other undesired isomers, comprising the steps of(a) diazotizing an aniline compound,(b) treating the diazonium salt with a salicylic acid ester compound blocked in the 3-position with an easily removed blocking group, preferably cloro,(c) removing the blocking group, and(d) hydrolyzing the ester to form the acid final product.

Abstract: 2-(3-Substituted amino-2-hydroxypropoxy)-3-substituted pyrazine compounds optionally having substituents in the 5 and/or 6 positions, possessing .beta.-adrenergic blocking properties are described. The products are prepared by reaction of a 2-chloro(or hydroxy)pyrazine with a 5-hydroxymethyl(or sulfonyloxymethyl)oxazolidine followed by acid hydrolysis.

Abstract: An efficient method has been found for the removal of the 3-isomer present in crude 9-(2-chloro-6-fluorobenzyl)adenine. Crude 9-(2-chloro-6-fluorobenzyl)adenine is transalkylated in sulfuric acid-toluene to reduce the 3-isomer to undetectable levels (<100 ppm). Alternately, crude 9-(3-chloro-6-fluorobenzyl)adenine is first treated with dilute nitric acid to remove the bulk of the 3-isomer followed by transalkylation to sulfuric acid-toluene to reduce the 3-isomer to undetectable levels (<100 ppm). The overall yield for this purification is about 95% based on the 9-(2-chloro-6-fluorobenzyl)adenine content of the crude material. The resulting pure 9-(2-chloro-6-fluorobenzyl)adenine has anticoccidial activity and is useful in controlling cecal and/or intestinal coccidiosis when administered in minor quantities to animals, in particular to poultry usually in admixture with animal sustenance.

Abstract: Fluorinated anilines, especially p-fluoroaniline and 2,4-difluoroaniline, are prepared by treating aromatic azides with anhydrous hydrogen fluoride. The aromatic azides, in turn, are prepared from the corresponding anilines by treatment with nitrous acid or salt thereof and an alkali metal azide in the presence of a mineral acid, and in an aqueous-nonaqueous, two-phase environment.

Abstract: A method of preparing 2,4-difluoroaniline by reacting 2,4,5-trichloronitrobenzene with a fluorinating agent in the presence of a solid-liquid phase interface, and utilizing a phase transfer catalyst to form 2,4-difluoro-5-chloronitrobenzene, followed by hydrogenation with hydrogen in the presence of a hydrogenation catalyst to form 2,4-difluoroaniline.

Abstract: The invention relates to an improved method of preparing salicylic acid and derivatives from phenyl esters which comprises the step of fusing acetoxyphenyl, or derivative suitable for preparing the desired salicylic acid derivative, with M.sub.2 CO.sub.3 where M is potassium or sodium in the presence of carbon dioxide, at a temperature of from 150.degree. to 250.degree. C., and at a pressure of from atmospheric to 500 p.s.i.g.

Abstract: 9-(Dihalobenzyl)adenines are prepared uncontaminated with other positional isomers in a series of mild transformations starting from 4,5,6-triaminopyrimidine and proceeding via 7-(N-formyl-N-dihalobenzyl)amino[1,2,5]-thiadiazolo[3,4-d]pyrimidine. The resulting compounds have anticoccidial activity and are useful in controlling cecal and/or intestinal coccidiosis when administered in minor quantities to animals, in particular to poultry usually in admixture with animal sustenance.