二芳基环丙烯酮与二芳基硫杂环丙烯1,1-二氧化物环加成反应制得的避孕药物。

Contraceptive agents from cycloaddition reactions of diarylcyclopropenones and diarylthiirene 1, 1-dioxides.

作者信息

Rosen M H, Fengler I, Bonet G, Steinetz B G, Giannina T, Dopick F R, Butler M C

出版信息

J Med Chem. 1976 Mar;19(3):414-9. doi: 10.1021/jm00225a016.

Abstract

The potential for compounds with antifertility activity from the reactions of diphenylcyclopropernone (1) and 2, 3-diphenylthiirene 1, 1-dioxide (2) with enamines is described. In certain instances, a marked dissociation of antifertility from estrogenic activity was possible. Two series were studied extensively, one was stilbene amides (7) and the other stilbene amino ketones (8). The latter series (8) afforded several materials from which, on further biological work-up, was singled out compound 21 as a potent antifertility agent in rats and hamsters.

摘要

本文描述了二苯基环丙烷酮（1）和2,3 - 二苯基硫杂环丙烯1,1 - 二氧化物（2）与烯胺反应生成具有抗生育活性化合物的可能性。在某些情况下，抗生育活性与雌激素活性可能会有明显分离。对两个系列进行了广泛研究，一个是芪酰胺（7）系列，另一个是芪氨基酮（8）系列。后一系列（8）得到了几种物质，经过进一步的生物学处理，从中挑选出化合物21作为大鼠和仓鼠的强效抗生育剂。