Synthesis of thieno [2, 3-b] azepin-4-ones as potential antineoplastic agents

RF Koebel, LL Needham…

Index: Koebel,R.F. et al. Journal of Medicinal Chemistry, 1975 , vol. 18, # 2 p. 192 - 194

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Citation Number: 23

Abstract

In view of the antitumor activity reported for 7, 8-dimethylbenzo [b] azepine-2, 5-dione, new isosteric thieno [2, 3-b]-azepin-4-ones have been prepared by a Dieckmann ring closure reaction. Substituted 2-amino-3-carbethoxythiophenes were tosylated, or benzoylated, and the corresponding sodium salt was alkylated with ethyl 4-bromobutyrate. The resulting product was cyclized in the presence of sodium hydride, and the azepinones were ...