维甲酸X受体拮抗剂HX-531的合成工艺优化  

Improved Synthesis of RXR Antagonist HX-531

作　　者：范文进[1] 吴之波 周林波[1] 陈国良[1] 

机构地区：[1]沈阳药科大学基于靶点的药物设计与研究教育部重点实验室,辽宁沈阳110016

出　　处：《精细化工中间体》2016年第1期57-60,共4页Fine Chemical Intermediates

摘　　要：以邻硝基苯胺和2-溴-5,5,8,8-四甲基-5,6,7,8-四氢萘为原料,经缩合、取代、还原、酰化、环合得到关键中间体4-(5,7,7,10,10-五甲基-7,8,9,10-四氢-5H-苯并[b]萘并[2,3-e][1,4]二氮杂-12-基)苯甲酸甲酯,再经硝化、水解得到目标产物4-(5,7,7,10,10-五甲基-2-硝基-7,8,9,10-四氢-5H-苯并[b]萘并[2,3-e][1,4]二氮杂-12-基)苯甲酸,反应总收率为24.7%,目标化合物结构经1H NMR和ESIMS谱确证。HX-531 was synthesized through eight steps using 2-nitroaniline and 2-bromo-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalene as the raw material. The structures of the target compound and key intermediates were confirmed by -1H NMR and MS spectra. The total yield reached 30%（calculated by 2-nitroaniline）. Compared with the route reported in literatures, the improved process has several advantages such as reducing pollution,Saving raw materials, getting a higher yield.

关 键 词：邻硝基苯胺 2-溴-5 5 8 8-四甲基-5 6 7 8-四氢萘 RXR拮抗剂 HX-531 

分 类 号：R914[医药卫生—药物化学]