氟伐他汀中间体3-(4-氟苯基)-1-(1-异丙基)-1H-吲哚的合成

Synthesis of Fluvastatin Intermediate 3-(4-Fluorophenyl)-1-(1-isopropyl)-1H-indol

以苯胺为原料,经异丙基化、与2-氯-1-(4-氟苯基)乙酮缩合、催化分子内环合制得合成氟伐他汀的关键中间体——3-(4-氟苯基)-1-(1-异丙基)-1H-吲哚,总收率高于90%,其结构经1HNMR确证。

A key intermediate of synthesizing fluvastatin,3-（4-fluorophenyl）-1-（1-isopropyl）-1H-indol（1）,was synthesized from aniline via iso-propylation with iso-propyl bromide,alkylation with 2-chloro-1-（4-fluorophenyl）ethanone,and then catalyzed intramolecular cyclization by heteropolyacid in overall yield more than 90%.The structure was confirmed by 1H NMR.