Synthesis and biological properties of thiophene ring analogs of mianserin

JWH Watthey, T Gavin, M Desai, BM Finn…

Index: Watthey; Gavin; Desai; Finn; Rodebaugh; Patt Journal of medicinal chemistry, 1983 , vol. 26, # 8 p. 1116 - 1122

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Citation Number: 17

Abstract

The synthesis of two thiophene-containing analogues of mianserin, Le., 1, 2, 3, 4, 10, 13b- hexahydro-2-methyl-piperazine [1, 2-a] thieno [2, 3-c][llbenzazepine (2), and the corresponding [3, 2-c] isomer (12) is described. The key step in the synthesis is the nucleophilic aromatic substitution reaction of the N-lithio derivative of l-methyl-3-(2-thieny1) piperazine (4) with the oxazoline derivative of o-anisic acid (7) to give the N- ...