A. H. Robins Company, Incorporated

Robert Louis Duncan, Jr

Robert Frederick Boswell, Jr

Robert F Boswell

1-Substituted-3-aminoethoxypyrrolidines having the formula ##STR1## WHEREIN R is benzyl, 2-ethoxyphenoxylower-alkyl, 2-propionyloxy-ethyl, 2-methoxy-4-acetylphenoxylower-alkyl, 4-fluorophenoxy lower alkyl, benzoyloxylower-alkyl, 3,4,5-trimethoxybenzoyloxylower-alkyl, 3,4,5-trimethoxybenzoyl, N-(4-methoxyphenyl) carbamoyl, 2-methoxyphenoxylower-alkyl, 3,4,5-trimethoxyphenyl-acetyl, 2-piperidinoethyl or carbamoyl, and Am is dilower-alkylamino, morpholino or piperidino having hypotensive properties are disclosed.

1-Substituted-3-aminoethoxypyrrolidines and use thereof

1-Substituted-3-aminoethoxypyrrolidines possessing hypotensive properties are disclosed. The compounds are prepared from 3-aminoethoxypyrrolidines.

1-Substituted-3-aminoethoxypyrrolidines

Novel 1-substituted-4-benzylpiperidines having .alpha.-substituents on the 4-benzyl moiety useful as anti-inflammatory agents, sedatives, and tranquilizers are represented by the formula ##STR1## wherein R represents acetyl, aryloxyloweralkyl, aroylloweralkylcarbamoyl, N-lower-alkylcarbamoyl, N,N-dilower-alkylcarbamoyl, N-arylcarbamoyl, N-(.omega.-nitrogen containing heterocycle)lower-alkylcarbamoyl, N(-.omega.-aminolower-alkyl)carbamoyl, 2-hydroxy-3-(o-methoxyphenoxy)propyloxycarbonyl, 2-carbamoylethyl, or 4-(p-fluorobenzoyl)piperidinoethyl; R.sup.1 represents hydrogen or hydroxy; R.sup.2 represents phenyl, p-fluorophenyl, m-trifluoromethylphenyl or cyclohexyl; Y represents hydrogen or fluorine with the proviso that when Y is hydrogen and R.sup.2 is phenyl, R is other than aroylloweralkyl. The pharmaceutically acceptable acid addition salts of the basic compounds of Formula I are included as part of the invention.

1-Substituted-4-benzylpiperidines

Novel 1-substituted-4-benzylpiperidines having .alpha.-substituents on the 4-benzyl moiety useful as antiinflammatory agents, sedatives, and tranquilizers are represented by the formula ##SPC1## Wherein R represents acetyl, aryloxyloweralkyl, aroylloweralkylcarbamoyl, N-lower-alkylcarbamoyl, N,N-dilower-alkylcarbamoyl, N-arylcarbamoyl, N-(.omega.-nitrogen containing heterocycle)lower-alkylcarbamoyl, N-(.omega.-aminolower-alkyl)carbamoyl, 2-hydroxy-3-(o-methoxyphenoxy)propyloxycarbamoyl, 2-carbamoylethyl, or 4-(p-fluorobenzoyl)piperidinoethyl; R.sup.1 represents hydrogen or hydroxy; R.sup.2 represents phenyl, p-fluorophenyl, m-trifluoromethylphenyl or cyclohexyl; Y represents hydrogen or fluorine with the proviso that when Y is hydrogen and R.sup.2 is phenyl, R is other than aroylloweralkyl. The pharmaceutically acceptable acid addition salts of the basic compounds of Formula I are included as part of the invention.

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Richmond, VA, United States of America

Robert Louis Duncan, Jr