第 47 卷第 5 期 Vol. 47 No. 5 2017 年 10 月 Oct 2017

所属栏目：医药及中间体 1-苯基环丙基甲腈及衍生物的合成

王晓丽1，褚朝森1，2*，胡玉涛1，李天雪2，王 政3 （1. 江苏联合职业技术学院 连云港中医药分院，江苏 连云港222007；2. 连云港市药物研发共性技术中心，江苏 连云港222007；3. 连云港康诚生物科技有限公司，江苏 连云港222007）

摘　要：合成了1-苯基环丙基甲腈及其衍生物。以苯乙腈为研究模型，考察了超声功率、温度、搅拌速率、时间对反应的影响，优化反应条件为：超声功率300 W、反应温度25℃、搅拌速率150 rpm、反应时间1.5 h，此时苯乙腈转化率达99.5%、产物收率达99.2%。该体系应用于1-苯基环丙基甲腈衍生物的合成，原料转化率≥92.3%，产物选择性≥92.2%。该体系用于杂环腈的转化，以噻吩-2-乙腈为原料合成了1-（噻吩-2-基）环丙烷甲腈，原料转化率为95.2%，产物选择性为97.8%。

关键词：超声波；四丁基溴化铵；1-苯基环丙基甲腈

中图分类号：R97　　文献标识码：A　　文章编号：1009-9212（2017）05-0028-04

Synthesis of 1-Phenyl-1-cyclopropanecarbonitrile and Its Derivatives

WANG Xiao-li1, CHU Chao-sen1, 2, HU Yu-tao1, LI Tian-xue2, WANG Zheng3 (1. Lianyungang TCM Branch of Jiangsu Union Technical Institute，Lianyungang 222007, China; 2. Lianyungang Common Technological Center for Drug Research and Development, Lianyungang 222007, China; 3. Lianyungang Kang Cheng Biological Technology Co., LTD., Lianyungang 222007, China)

Abstract：1-Phenyl-1-cyclopropanecarbonitrile and its derivatives were synthesized. Taking phenylacetonitrile as an example, the reaction conditions including ultrasonic power, temperature, stirring speed, and reaction time were studied. The experimental data showed that the optimum reaction conditions were as followings: 300 W, 25℃, 150 rpm, 1.5 h. A yield of 99.2% with a conversion of 99.5% was achieved. A variety of phenylacetonitrile derivatives were also synthesized with high conversion (≥92.3%) and selectivity (≥92.2%). This method was also applied in the transformation of heterocyclicnitrile. 2-Thiopheneacetonitrile used as the starting material, the 1-(thiophen-2-yl)cyclopropanecarbonitrile was synthesized with a conversion of 95.2% and a selectivity of 97.8%.

Key words：ultrasonic; TBAB; 1-phenyl-1-cyclopropanecarbonitrile

基金项目：江苏省青蓝工程培养基金项目（2014），连云港市521人才项目（2015）

作者简介：王晓丽（1982-），女，河南永城人，硕士，讲师，研究方向：药物分析。

联 系 人：褚朝森，副教授，硕士，研究方向：生物有机合成（E-mail：chuchaosen@126.com）。

收稿日期：2017-09-29