维兰特罗关键中间体合成新方法

摘要

维兰特罗三苯乙酸盐(Vilanterol trifenatate)是由葛兰素史克公司(GSK)开发的长效β2受体激动剂.(R)-5-(2,2-二甲基-4H-1,3-苯并二氧芑-6-基)-1,3-噁唑烷-2-酮是关键中间体,文章基于已有的合成方法,提出一条新的路线.所得的目标化合物都经核磁共振氢谱确定结构,总收率达50 %.%Vilanterol trifenatate is a long-acting β2 adrenoceptor agonist developed by the GSK.(R)-5-(2,2-dimethyl-4H-1,3-benzodioxine-6-yl)-1,3-oxazolidine-2-ketone is the key intermediate, the paper proposes a new one based on existing methods.The structure of the intermediate was characterized by 1H NMR.The overall yield of the synthetic route was 50 %.