Tetrahedron

Polycondensed heterocycles. IX. Pyrrolo [2, 1-c][1, 4] benzothiazepines. Synthesis of 3-(dimethylamino) methyl derivatives

A Garofalo, G Campiani, SM Ciani, I Fiorini, V Nacci

Index: Garofalo, Antonio; Campiani, Giuseppe; Ciani, Silvia M.; Fiorini, Isabella; Nacci, Vito Tetrahedron, 1996 , vol. 52, # 22 p. 7745 - 7754

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Citation Number: 5

Abstract

The synthesis of 3-(dimethylamino) methyl-5H, 11H-pyrrolo [2, 1-c][1, 4] benzothiazepine derivatives 2a-c, which might show significant central nervous system (CNS) activity, is described. The basic side chain was introduced by a Mannich condensation with the preformed heterocyclic systems 1a-c. Synthesis of novel 5-phenyl-5H, 11H-pyrrolo [2, 1-c][1, 4] benzothiazepine 1c by a nucleophilic aromatic fluoride displacement-cyclization and an ...