孕酮受体拮抗剂ZK98299衍生物的合成

Synthesis of Progesterone Receptor Antagonist ZK98299 Derivatives

为寻找新的、活性强且毒副作用小的孕酮受体拮抗剂，本文对孕酮受体拮抗剂ＺＫ９８２９９（４ｂ）的Ｃ_（１７）边链进行结构改造，合成了６个ＺＫ９８２９９衍生物：（２ａ）；（２ｂ）．（３）．（５ａ），（５ｂ），（６），除化合物（６）外，均未见文献报道，经光谱确证其结构，化合物（２ｂ）经初步体外药理试验，显示对大鼠蜕膜细胞的作用略强于ＺＫ９８２９９．

In order to search for novel progesterone receptor antagonists with higher efficiency and less side effects,the structure of progesterone receptor antagonist ZK98299(4b)at C_17-substitute was modified.Six ZK98299 derivatives were synthesized.The compounds (2a).(2b).(3),(5a) and (5b)have not been reported in the literature.The effect of the compound (2b)on decidual cells of rats was a little more active than ZK98299.