| 盐酸昂丹司琼有关物质B的合成 |
| |
| 引用本文： | 高虎,熊路,刘海涛,吴松,童元峰.盐酸昂丹司琼有关物质B的合成[J].中国医药工业杂志,2011,42(10). |
| |
| 作者姓名： | 高虎 熊路 刘海涛 吴松 童元峰 |
| |
| 作者单位： | 中国医学科学院北京协和医学院药物研究所,卫生部天然药物生物合成重点实验室,北京100050 |
| |
| 基金项目： | 临床用药安全检测技术标准的研究 |
| |
| 摘 要： | 为了盐酸昂丹司琼的质控,合成了欧洲药典7.0中规定的有关物质B6,6′-亚甲基双9-甲基-3-(2-甲基-1H-咪唑-1-基)甲基]-1,2,3,9-四氢-4H-咔唑-4-酮]]:用4,4′-二氨基二苯甲烷经重氮化及还原得到4,4′-二肼基二苯甲烷二盐酸盐,与1,3-环己二酮缩合后进行Fischer环合生成6,6′-亚甲基双(1,2,3,9-四氢4H-咔唑-4-酮),再经甲基化、与多聚甲醛进行羟醛缩合反应,最后与2-甲基咪唑进行Michael加成制得.
|
| 关 键 词： | 盐酸昂丹司琼 有关物质 止吐药 对照品 合成 |
Synthesis of Related Substance B of Ondansetron Hydrochloride |
| |
| Authors: | GAO Hu XIONG Lu LIU Haitao WUSong TONG Yuanfeng |
| |
| Institution: | GAO Hu,XIONG Lu,LIU Haitao,WU Song,TONG Yuanfeng~* (Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Key Lab.of Biosynthesis of Natural Pharmaceutical Products,Ministry of Health of PRC,Beijing 100050) |
| |
| Abstract: | To perform the quality control of ondansetron hydrochloride,the related substance B,i.e.6,6'- methylene-bis-9-methyl-3-(2-methyl-1H-imidazol-1-yl)methyl]-1,2,3,9-tetrahydro-4H-carbazol-4-one]recorded in EP 7.0,was synthesized from 4,4'-diaminodiphenylmethane by diazotization and reduction to give 4,4'-dihydrazinodi-phenylmethane dihydrochloride,which was subjected to condensation with 1,3-cyclohexanedione and Fischer cyclization to form 6,6'-methylene-bis-(l,2,3,9-tetrahydro-4H-carbazol-4-one),followed by... |
| |
| Keywords: | ondansetron hydrochloride related substance antiemetics reference substance synthesis |
| 本文献已被 CNKI 万方数据 等数据库收录！ |
|
