新型3-取代8-氮杂双环[3,2,1]辛烷衍生物的合成与表征  

Synthesis and Representation of Novel 3-substituted 8-aza-bicyclo[3.2.1] octane Derivative

作　　者：覃宇[1] 

机构地区：[1]武汉职业技术学院生物工程学院,湖北武汉430074

出　　处：《武汉职业技术学院学报》2011年第5期103-106,共4页Journal of Wuhan Polytechnic

摘　　要：8-氮杂双环[3,2,1]辛烷衍生物是多种药物分子中的重要活性基团,特别是3位取代产物其药效更加明显。以2,5-二甲氧基四氢呋喃、3-羰基戊二酸、苄胺等为原料,通过环化、N保护、交叉偶合,合成了桥环上3位取代的产物8-N-叔丁氧羰基-3-硼酸频哪醇基-8-氮杂二环[3,2,1]-2-辛烯。其中间体产物和目标产物的结构经1H NMR、LC-MS和元素分析表征确认,为进一步后续反应形成药物分子奠定基础。8-aza-bicyclo[3.2.1] octane derivatives are important active groups in a variety of drug molecules,and the efficacy of 3-substituted products is especially obvious.In this paper,a 3-substituted 8-aza-bicycoloctane derivative,8-N-tert-butoxycarbony-3-pinacolatoboronyl-8-aza-bicyclo[3.2.1]-2-octene is synthesized by the cyclization,N-protection and cross coupling of 2,5-dimethoxyltetrhydrofuran,3-acetondicarboxylic acid and benzyl amine.The structures of intermediate products and target product are represented and confirmed by 1H NMR,LC-MS and elemental analysis,which forms the foundation for the synthesis of drug molecules in the following steps.

关 键 词：氮杂双环 拮抗剂 合成 表征 

分 类 号：Q81[生物学—生物工程]