非布司他中间体2-异丁氧基-5-溴苯甲腈的合成

Synthesis of 5-Bromo-2-Isobutoxybenzonitrile as A Key Intermediate of Febuxostat

以水杨醛为起始原料,经溴代、氰基化、烃化3步反应合成了2-异丁氧基-5-溴苯甲腈,总收率为47.7%,产品结构经1 HNMR和MS确证。该工艺原料易得、操作简单、成本较低,适合工业化生产。

5-Bromo-2-isobutoxybenzonitrile was synthesized with an overall yield of 47.7 % via a three-step procedure as bromination, cyanidation and alkylation, using salicyialdehyde as starting material. The structure of the product was confirmed by 1HNMR and MS. The process Was suitable for industrial preparation because of its advantages of mild reaction conditions ,facile operation and relatively lower cost.