Improvement of synthetic route of brivudine
10.11665/j.issn.1000-5048.20220106
- VernacularTitle:溴夫定的合成路线改进
- Author:
Xufeng WU
1
;
Shiying CHAI
;
Jianhong LIU
;
Zhihui WANG
;
Ruifeng YIN
;
Ruiwei CAO
;
Xinqiang SUN
Author Information
1. 浙江医药股份有限公司新昌制药厂
- Publication Type:Journal Article
- Keywords:
brivudine;
synthesis;
process improvement
- From:
Journal of China Pharmaceutical University
2022;53(1):41-45
- CountryChina
- Language:Chinese
-
Abstract:
This article summarizes and analyzes the reported synthetic routes of brivudine in patent and literature.2′-Deoxyuridine was employed as starting material, affording brivudine through iodization, heck coupling, hydrolysis, decarboxylation, bromination and recrystallization.After optimization of reaction conditions of each step, a synthetic route suitable for industrial production was achieved with simple synthetic process, high yield and excellent purity.
