多沙唑嗪的合成工艺改进

Improved Synthesis of Doxazosin

用邻碘苯酚为起始原料,经过亲核取代、还原、不对称合成、氧化、缩合等过程分别合成多沙唑嗪(Doxazosin)的消旋体以及其光学异构体((R)-Doxizosin)。目标化合物以及中间体的结构经1H NMR、13C NMR、MS谱等确证。方法操作简便,收率高,其中外消旋体和光学异构体收率分别为62.3%和66.4%,光学纯度92%。

The preparation of racemic and optical isomer of doxazosin from o-iodine phenol via nucleophilic substitution, reduction, asymmetric synthesis, oxidation and condensation processes was studied, by using o-iodine phenol as raw metarial. The structures of the target compounds and intermediates are were confirmed by ^1H NMR, ^13C-NMR and MS spectra. The procedure of the new synthetic method is simple with high yield. In a typical process, the optical product with was obtained the yield of in a yield of 66.4% withand the optical purity of 92%.