司替戊醇的合成  

Synthesis of Stiripentol

作　　者：赵杰[1] 张恺[1] 华圆[1] 程诚[2] 杜玉民[1] 

机构地区：[1]河北医科大学药学院,河北石家庄050017 [2]北京化工大学化学工程学院,北京100029

出　　处：《中国医药工业杂志》2013年第8期747-748,共2页Chinese Journal of Pharmaceuticals

基　　金：河北省自然科学基金项目(2012206125)

摘　　要：胡椒醛与甲基叔丁酮在相转移催化剂氯化苄基三丁铵催化下,室温进行Claisen-Schmidt反应制得4,4-二甲基-1-[(3,4-亚甲二氧基)苯基]-1-戊烯-3-酮,再经硼氢化钠还原得到抗癫痫药司替戊醇,总收率约85%。Stiripentol, an anti-epileptic drug, was synthesized from piperonal and 3,3-dimethylbutan-2- one by Claisen-Schmidt reaction in the presence of phase transfer catalyst benzyltributylammonium chloride to give 4,4-dimethyl-1- E （3,4-methylenedioxy） phenyl] -1-pentene-3-one, which was subjected to reduction using NaBH4 with an overall yield of about 85 %.

关 键 词：司替戊醇 抗癫痫药 细胞色素P450抑制剂 合成 

分 类 号：R971.6[医药卫生—药品]