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Centchroman是一新型非甾体女用口服避孕药,我们对其合成路线进行了改进。其中在FriedelCrafts烷基化反应中高选择性地获得反式异构体,从而避免了文献报道中的高压氢化和构型转化两个反应单元。共五步反应得到最终产物。收率达40%。
Centchroman is a new non-steroidal oral contraceptive for women and we have made improvements to its synthetic route. In the Friedel-Crafts alkylation reaction, trans isomers are obtained with high selectivity, thus avoiding the two reaction units of high-pressure hydrogenation and configuration conversion reported in the literature. A total of five reactions gave the final product. Yield 40%.