异维A酸衍生物合成与结构表征  

Synthesis and Characterization of 13-cis-Retinoic Acid Derivatives

作　　者：向建南[1] 陈超越[1] 刘志常[1] 曾勇 党奎峰[1] 邓小强[1] 尹霞[1] 

机构地区：[1]湖南大学化学化工学院,湖南长沙410082 [2]汉寿正阳有限公司,湖南汉寿415900

出　　处：《湖南大学学报（自然科学版）》2004年第4期6-10,共5页Journal of Hunan University:Natural Sciences

基　　金：教育部留学归国人员基金(No.2003406);湖南省自然科学基金(No.02JJY4009和03JJY3016)资助项目

摘　　要：在考察了不同的反应条件后,建立了以二环己基碳酰亚胺(DCC)为脱水剂、合成具有药物活性的异维A酸酯和异维A酰胺的合成方法。在温和条件下(0℃至室温)以4-二甲氨基吡啶(DMAP)为催化剂,将在通常情况下极易异构化的异维A酸3能顺利地转化为它们的衍生物,收率为42.3%～82.4%。合成了10种尚未见文献报道的异维A酸酯和异维A酰胺,并考察了它们的分离纯化条件,以1H,13CNMR和MS对它们的结构进行了表征。After investigating various reaction conditions, a new method, with dicyclohexylcarbodiimide (DCC) as the reagent, was built to synthesize pharmaceutically active retinoates and retinamides. With 4-dimethylaminopyridine (DMAP) as the catalyst, the compound 3, which is very easily isomerized under general reaction conditions, was conveniently inverted to relative derivatives under mild reaction conditions. The yields were 42.3%～82.4%. Ten retinoates and retinamides not yet published in existing literatures were synthesized. The conditions to purify them were evaluated and their structures were characterized by means of ()~1H, ()^(13)C NMR and MS.

关 键 词：异维A酸 类维生素A 异维A酸酯 异维A酰胺 表征 

分 类 号：O621.33[理学—有机化学]