氟伐他汀中间体3-(4-氟苯基)-1-异丙基-1H-吲哚的合成新工艺

The new synthetic technology of fluvastatin intermediate 3-(4-Fluorophenyl)-1-isopropyl-1H-indol

目的设计一条氟伐他汀中间体3-(4-氟苯基)-1-异丙基-1H-吲哚的合成新路线。方法以苯胺为原料,经异丙基化,环合2步反应合成氟伐他汀中间体。结果目标化合物的结构经1H-NMR确证,总收率为83.5%,比文献收率提高了33.5%。结论改进后的方法操作简便,有利于工业化生产。

Objective To design a new synthetic route of the fluvastatin intermediate 3 - （ 4 - Fluorophenyl ） - 1 - isopropyl - 1H - indol. Methods Aniline was used as raw material and the fluvastatin intermediate was synthesized by isopropylation and cyelization reaction. Results The structure of target compound was confirmed by 1 H - NMR and the overall yield was 83.5%. Compared with literatures, the overall yield was raised by 33.5%. Conclusion This synthetic method was convenient and suitable for industrial production.