微波辅助合成氟曲马唑  

Synthesis of flutrimazole under microwave irradiation

作　　者：张玲[1] 安顺永 刘玲[1] 李晨光[1] 刘毅[1] 

机构地区：[1]徐州医学院药学院,江苏徐州221004 [2]徐州市化工研究所,江苏徐州221004

出　　处：《化学试剂》2010年第10期933-936,954,共5页Chemical Reagents

基　　金：江苏省自然科学基金资助项目(BK2009523);江苏省高校自然科学基金资助项目(09KJB350003);江苏省高校自然科学基金资助项目(08KJD530004);徐州市科技计划项目(XM08C059);徐州医学院肿瘤生物治疗实验室资助项目(CO903)

摘　　要：以2-氟二苯甲酮和对氟溴苯为原料,经格氏反应、卤代反应、N-烷基化反应得到抗真菌药氟曲马唑,产物纯度99.7%以上,总收率65.8%(以2-氟二苯甲酮计)。探讨了以乙酰氯作为卤代试剂的卤代反应以及微波辅助的N-烷基化反应的最佳合成条件,产物结构经熔点、元素分析、IR和1HNMR确证。改进后的工艺简便、高效,收率以及产物纯度均提高。Flutrimazole,an antifungal agent,was synthesized from 2-fluorobenzophenone and p-fluorobromobenzene,via the Grignard reaction,halogenation and N-alkylation in an overall yield of 65.8%（based on 2-fluorobenzophenone） with a product purity of over 99.7%.The synthetic procedure was optimized.The halogenation reaction with acetyl chloride and the N-alkylation reaction under microwave irradiation were explored.The structure of the title compound was confirmed by melting point measurement,elemental analysis,IR and 1HNMR.The improved synthetic route was convenient and effective,and the yield and purity of the title product were all improved.

关 键 词：氟曲马唑 微波辐射 N-烷基化反应 卤代反应 

分 类 号：R914.5[医药卫生—药物化学]