American Home Products Corporation

George C Buzby, Jr

Thomas J Colatsky

Ronald J McCaully

Michael W Winkley

Henry G Schouten

This invention provides Class III anti-arrhythmic agents of the formula: ##STR1## in which R.sup.1 is alkylsulfonamido, R.sup.2 is ethyl, R.sup.3 is hydrogen, R.sup.4 is ethyl, and n is 2 to 4, or a pharmaceutically acceptable salt thereof.

Anti-arrhythmic agents

N-Aminoalkyl(perfluoroalkanoylaminophenyl)sulfonic acid amides of the formula: ##STR1## in which R.sup.1 is perfluoroalkanoylamino of 2 to 4 carbon atoms, in 3- or 4- position of the benzene ring;

N-aminoalkylperfluoroalkanoylaminobenzene-sulfonamide anti-arrhythmic

Disclosed herein is a process for producing an asymmetric indoline-2-carboxylic acid of the structural Formula: ##STR1## wherein X is hydrogen, bromine, chlorine, C.sub.1-4 alkyl or C.sub.1-4 alkoxy, which comprises:

Process for the asymmetric synthesis of chiral

This invention provides Class III anti-arrhythmic agents of the formula: ##STR1## in which R.sup.1 is alkylsulfonamido, arylsulfonamido, perfluoroalkylsulfonamido, R.sup.2 and R.sup.3 are hydrogen or alkyl, R.sup.4 is alkyl, and n is 2 to 4, or a pharmaceutically acceptable salt thereof.

Alkylsulfonamido or perfluoroalkylsulfonamido benzenesulfonamides

This invention provides a group of anti-arrhythmic agents of the formula: ##STR1## in which R.sup.1 is hydrogen, hydroxy, alkoxy or halo;

N-(aminoalkylene)benzenesulfonamides

N-Aminoalkyl(aminophenyl)sulfonic acid amides of the formula: ##STR1## in which R.sup.1 is --NH.sub.2, alkylamino of 1 to 3 carbon atoms or alkanoylamino of 2 to 4 carbon atoms, in 3- or 4-position of the benzene ring;

4-amino benzenesulfonamides

Compounds presenting the following structural formula: ##STR1## in which the nitro substituent is in 3 or 4 position of the phenyl ring; R.sup.1 is hydrogen or alkyl;

N-substituted-4(3)-nitrobenzene sulphonamides

Process for the asymmetric synthesis of chiral indoline-2-carboxylic

Compounds of the formula: ##STR1## in which Z is ##STR2## where R is hydrogen, alkyl, polyfluorinated alkyl, --CN, cyanoalkyl, cycloalkyl or cycloalkylalkyl;

An anti-arrhythmic agent which is N-[3-[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-N-(1-methylethyl)- 2,3,4-trimethoxy-benzenesulfonamide or a pharmaceutically acceptable salt thereof.

Disclosed herein is a process for the preparation of optically active compounds of the formula: ##STR1## in which R is a lower alkyl, lower alkoxy, benzyloxy, phenyl, o-nitrophenyl, p-nitrophenyl, or p-tolyl group, or salts or esters thereof, which process comprises the following steps:

Resolution of 3-benzoylthio-2-methyl-propanoic acid with

Compounds of the formula: ##STR1## in which Y is --(CH.sub.2).sub.n -- where n is one of the integers 1,2,3 or 4 or ##STR2## where R is hydrogen, alkyl, polyfluorinated alkyl, --CN, cyanoalkyl, cycloalkyl or cycloalkylalkyl;

Described herein is a process for separating the enantiomers of (+)-2,3-dihydroindole-2-carboxylic acid, which process utilizes (+) or (-)-ephedrine as the resolving agent. The resolved acids are useful as intermediates in the preparation of angiotensin converting enzyme inhibitors.

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Blue Bell, PA, United States of America

George C Buzby, Jr