阿利克仑中间体的合成及提纯

Synthesis and Purification of the Intermediates of the Aliskiren

以异香草醛为原料通过醚化、还原、甲基醚化、溴代、亲电取代、氧化、还原等多步法合成阿里克伦中间体1-氯-2R-[4-甲氧基-3-(3-甲氧基丙氧基)苄基]-3-甲基丁烷粗品,粗品采用柱层析法分离,分离得到阿利克仑中间体纯度为98.3%,回收率达90.4%。通过实验室合成及建立较简单的分离工艺,为工业生产、提纯阿利克仑中间体提供了可靠的实验依据。

Using isovanillin as raw material , through the reduction of etherification , methyl etherification , bromination, oxidation, reduction, dear electricity multi step synthesis of aliskiren intermediate 1-chloro-2R-[4-methoxy-3 -（ 3 -methoxy propoxy ） benxyl ] -3 -methyl butane crude , crude product by column chromatography separation, separation of aliskiren intermediate purity was 98.3% and the recovery rate was 90.4%.Through the establishment of separation process synthesis and relatively simple laboratory , the reliable experimental basis was proposed for industrial production and purification of aliskiren intermediates.