比卡鲁胺不对称合成工艺研究

Asymmetric synthesis of bicalutamide

目的探索比卡鲁胺的不对称合成工艺。方法以L-脯氨酸为起始原料,经酰化、环合、水解、环合、缩合、环氧化、烃化、氧化8步反应制备比卡鲁胺。结果与结论总收率为31. 97%,产品结构经~1H-NMR和ESI-MS确证。该工艺原料易得、操作简单、成本较低,适用于工业化生产。

A new asymmetric synthetic route has been developed for the preparation of bicalutamide. Starting form L-proline,an 8-step procedure of acylation,cyclization,hydrolysis,cyclization,condensation,epoxidation, a lkylation and oxidation,was carried out to provide bicalutamide with an overall yield of 31. 97%. The structure was confirmed by 1H-NMR and MS. The process is scalable for industrial production for its advantages of short period,mild reaction conditions and relatively low cost.