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长效避孕药——醋炔诺醇环戊丙酸酯的合成
引用本文:陈炜,邱来康. 长效避孕药——醋炔诺醇环戊丙酸酯的合成[J]. 药学学报, 1984, 19(12): 935-937
作者姓名:陈炜  邱来康
作者单位:上海市计划生育科学研究所;**上海市医药局中等专科学校
摘    要:In order to prolong the biological action of norethisterone acetate (Ⅰ) we have synthesized its cyclopentylpropionic ester (Ⅳ). I was reduced to its hydroxy intermediate (Ⅱ) by potassium borohydride in 91% yield and then esterifled with cyclopentyl chloride to give Ⅳ in 49% yield.A single intramuscular dose of 60 mg of cyclopentylpropionic ester of Norethisterone acetate was fo und to protect women from pregnancy for 3 months. The efficacy rate of the contraceptive effect in 1728 cases of clinical trials was about 99.6%.

关 键 词:醋炔诺醇  醋炔诺醇环戊丙酸酯
收稿时间:1983-12-30

SYNTHESIS OF CYCLOPENTYLPROPIONIC ESTER OF NORETHISTERONE ACETATE AS LONG ACTING CONTRACEPTIVES
CHEN Wei and QIU Lai-Kang. SYNTHESIS OF CYCLOPENTYLPROPIONIC ESTER OF NORETHISTERONE ACETATE AS LONG ACTING CONTRACEPTIVES[J]. Acta pharmaceutica Sinica, 1984, 19(12): 935-937
Authors:CHEN Wei and QIU Lai-Kang
Abstract:In order to prolong the biological action of norethisterone acetate (Ⅰ) we have synthesized its cyclopentylpropionic ester (Ⅳ). I was reduced to its hydroxy intermediate (Ⅱ) by potassium borohydride in 91% yield and then esterifled with cyclopentyl chloride to give Ⅳ in 49% yield.A single intramuscular dose of 60 mg of cyclopentylpropionic ester of Norethisterone acetate was fo und to protect women from pregnancy for 3 months. The efficacy rate of the contraceptive effect in 1728 cases of clinical trials was about 99.6%.
Keywords:cyclopentylpropionic ester of norethisterol acetate  Norethisterol acetate
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