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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%。
Androst-4-ene-3,17-dione by enol etherification reaction of 3-ethoxy androst-3,5-dienoandrost-17-one, and paraformaldehyde and N- Mannich reaction of aniline can give 6- (N-methyl-N-phenyl) aminomethyl-4-ene-3,17-androstane dione, and then by elimination reaction, 6-methylene- -ene-3,17-androstane-dione, and finally oxidized to exemestane for a total yield of about 42%.