碘代咔唑类DNMT抑制剂中间体的合成  

Synthesis of DNMT Inhibitor Intermediate with Iodine Substituted Carbazole

作　　者：潘琪[1] 王凯[1] 莫灿[1] 周文[1] 刘博[1] PAN Qi WANG Kai MO Can ZHOU Wen LIU Bo(The Second Clinical Medical College, Guangzhou University of Chinese Medicine, Guangzhou 510006, China)

机构地区：[1]广州中医药大学第二临床医学院,广东广州510006

出　　处：《化学试剂》2017年第2期195-198,共4页Chemical Reagents

基　　金：国家自然科学基金资助项目(81202398);广东省科技计划项目(2013B010102006;2014A020221035;2015A020211025);广东省中医院中医药科学技术研究专项项目(YN2014ZHR209;YN2015MS03);国家中医药管理局临床基地科研专项项目(JDZX2015207)

摘　　要：以咔唑和碘为原料,经碘化、N-烷基化、开环得到目标化合物1,3-双(3,6-二碘-9H-咔唑-9-基)-2-丙醇,总收率36.5%。产物的结构经~1HNMR、^(13)CNMR和MS表征。对基于I_2/DMSO体系的关键碘化反应进行了机理阐释和条件优化,确定了最优反应条件为n(咔唑)∶n(I_2)=2∶3,110℃下反应4 h,平均产率为85.2%。1,3-Bis（3,6-diiodo-9H-carbazol-9-yl） propan-2-ol was synthesized from carbazole and iodine by iodination,N-alkylation and ring-opening. The total yield is 36. 5%. The target compounds were confirmed with-1HNMR,-（13）CNMR and MS. The mechanism of the key iodination based on the I_2/DMSO system was explained and the condition of iodination was optimized. In the presence of n（carbazole） ∶ n（I_2） = 2∶ 3 as starting materials,DMSO as solvent,4 h under 110 ℃,the average yield of the iodination was up to 85. 2%.

关 键 词：DNMT抑制剂 1 3-双(3 6-二碘-9H-咔唑-9-基)-2-丙醇 3 6-二碘咔唑 碘代 合成 

分 类 号：TQ251.3[化学工程—有机化工]