A convenient synthesis of cis and trans-(±)-4-amino-1-[2-(hydroxylmethyl)-1,3-oxathiolan-5-yl]-2(1H)-pyrimidinone

被引：0

作者：

Shen, Y ^{[1
]}

Xiang, L ^{[1
]}

Deng, Y ^{[1
]}

Zhong, YG ^{[1
]}

机构：

[1] Sichuan Univ, W China Sch Pharm, Dept Med Chem, Chengdu 610041, Peoples R China

来源：

CHINESE CHEMICAL LETTERS | 2006年 / 17卷 / 04期

关键词：

lamivudine; geometrical isomer; cis-(+/-) isomer; trans-(+/-) isomer; synthesis;

D O I：

暂无

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A convenient synthesis of cis-(+/-) isomer 1 and trans-(+/-) isomer 2 of lamivudine starting from benzoyloxyacetaldehyde and 1,4-dithiane-2,5-diol is described. The key steps include chlorination of oxathiolane lactol 5 by SOCl2/DMF, followed by coupling with silylated N-4-acetylcytosine and deprotection. The overall yield was 42.6% and 20.1%, respectively.

引用

页码：431 / 433

页数：3

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