| 缬沙坦的合成 |
| |
| 引用本文： | 王晓东,郭晔堃,潘璐,黄素萍. 缬沙坦的合成[J]. 中国医药工业杂志, 2012, 43(6): 416-418 |
| |
| 作者姓名： | 王晓东 郭晔堃 潘璐 黄素萍 |
| |
| 作者单位： | 1. 常州四药制药有限公司,江苏常州,213004
2. 中国医药工业研究总院上海医药工业研究院,创新药物与制药工艺国家重点实验室,上海200437 |
| |
| 摘 要： | N-[(2’-氰基联苯-4-基)甲基]-L-缬氨酸甲酯,与正戊酰氯在甲苯中,以DMAP作催化剂、碳酸钠作缚酸剂进行酰化反应制得N-(1-氧代戊基)-N-[(2’-氰基联苯-4-基)甲基]-L-缬氨酸甲酯,再在相转移催化剂双三甲基硅烷化聚乙二醇400(4)作用下与叠氮钠反应成四唑后,经水解制得抗高血压药缬沙坦,总收率约75%。
|
| 关 键 词： | 缬沙坦 抗高血压药 合成 |
Synthesis of Valsartan |
| |
| WANG Xiaodong , GUO Yekun , PAN Lu , HUANG Suping. Synthesis of Valsartan[J]. , 2012, 43(6): 416-418 |
| |
| Authors: | WANG Xiaodong GUO Yekun PAN Lu HUANG Suping |
| |
| Affiliation: | 1(1.Changzhou Siyao Pharmaceuticals Co.,Ltd.,Changzhou 213004;2.State Key Lab.of New Drug & Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry,China State Institute of Pharmaceutical Industry,Shanghai 200437) |
| |
| Abstract: | Valsartan was synthesized from N-[(2’-cyanobiphenyl-4-yl)methyl]-L-valine methyl ester by acylation with n-pentanoyl chloride in toluene with DMAP as catalyst and Na2CO3 as base to give N-(1-oxopentyl)-N-[(2’-cyanobiphenyl-4-yl)methyl]-L-valine methyl ester,which was subjected to reaction with sodium azide with Bis(trimethylsilyl)-PEG 400(4) as PTC to form the tetrazole,followed by hydrolysis with an overall yield of about 75%. |
| |
| Keywords: | valsartan antihypertensive synthesis |
| 本文献已被 CNKI 万方数据 等数据库收录！ |
|
