摘要
雄甾-4-烯-3,17-二酮经烯醇醚化反应制得3-乙氧基雄甾-3,5-二烯雄甾-17-酮,再与多聚甲醛和N-甲基苯胺进行Mannich反应可得6-(N-甲基-N-苯基)氨甲基-4-烯-3,17-雄甾二酮,然后经消除反应可得6-亚甲基-4-烯-3,17-雄甾二酮,最后经氧化得到依西美坦,总收率约42%。
Exemestane was synthesized from 4-androstene-3,17-dione via enol etherification to give 3-ethoxyandrosta-3,5-dien-17-one, followed by Mannich reaction with paraformaldehyde and N-methylaniline to afford 6-（N-methyl-N-phenyl） aminomethyl-4-androstene-3,17-dione, which was subjected to elimination to give the key intermediate 6-methylene-androst-4-ene-3,17-dione, followed by oxygenation with an overall yield of about 42 %.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2017年第2期163-165,共3页
Chinese Journal of Pharmaceuticals
基金
国家自然科学基金(21176156)
浙江省公益技术研究工业项目(2015C31147)
