合成2-丁基-1,3-二氮杂螺4.4壬-1-烯-4-酮的工艺改进

摘要

以1-氨基环戊腈草酸盐为起始原料,经双氧水水解、戊酰氯酰化、环合制得厄贝沙坦的关键中间体——2-丁基-1,3-二氮杂螺[4.4]壬-1-烯-4-酮,总产率80.9％,其结构经1H NMR,13C NMR和MS确证.%Lrbesartan key intermediate, 2-butyl-l ,3-diazaspiro[4. 4] non-1-en4-one, was synthesized by a three-step reaction of hydrolyzation, acylation and cyclization in total yield of 80.9%. The structure was confirmed by 1H NMR, 13C NMR and MS.