依巴斯汀的合成工艺改进 |
| |
引用本文: | 孙平华,唐文生,张虎山,孙铁民.依巴斯汀的合成工艺改进[J].中国医药工业杂志,2004,35(6):326-327. |
| |
作者姓名: | 孙平华 唐文生 张虎山 孙铁民 |
| |
作者单位: | 1. 暨南大学药学院,广东,广州,510632 2. 沈阳药科大学制药工程学院,辽宁,沈阳,110015 |
| |
摘 要: | 用1-苄基-4-哌啶醇和二苯甲基溴经缩合、脱苄置换和水解反应制得4-二苯甲氧基哌啶,再与4-氯-1-(4-叔丁基苯基)-1-丁酮在碘化钾存在下缩合、成盐制得富马酸依巴斯汀,总收率36%.
|
关 键 词: | 依巴斯汀 H1-受体拮抗剂 合成 |
文章编号: | 1001-8255(2004)06-0326-02 |
Improved Synthesis of Ebastine |
| |
Authors: | SUN Ping-Hua TANG Wen-Sheng ZHANG Hu-Shan SUN Tie-Min |
| |
Institution: | SUN Ping-Hua1,TANG Wen-Sheng2,ZHANG Hu-Shan2,SUN Tie-Min2 |
| |
Abstract: | A new H1-receptor antagonist ebastine was synthesized from 1-benzyl-4-piperidinol by condensation withPh2CHBr, debenzylation, replacement and hydrolytic decarboxylation to give 4-benzhydryloxypiperidine followed byreaction with 1-(4-t-butylphenyl)-4-chloro-butan-1-one and salt formation with fumaric acid in an overall yield of 36%. |
| |
Keywords: | ebastine H1-receptor antagonist synthesis |
本文献已被 CNKI 维普 万方数据 等数据库收录! |
|