SYNTHESIS AND ANTIVIRAL EVALUATION OF ENANTIOMERIC 2',3'-DIDEOXY-2',3'-DIDEOXY-4'-THIONUCLEOSIDES AND 2',3'-DIDEHYDRO-2',3'-DIDEOXY-4'-THIONUCLEOSIDES

被引：52

作者：

YOUNG, RJ

SHAWPONTER, S

THOMSON, JB

MILLER, JA

CUMMING, JG

PUGH, AW

RIDER, P

机构：

[1] Department of Medicinal Chemistry, The Wellcome Foundation Ltd., Beckenham

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 22期

关键词：

D O I：

10.1016/0960-894X(95)00472-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and antiviral evaluation of 2',3'-dideoxy and 2',3'-didehydro-2',3'-dideoxy 4'-thionucleosides in both enantiomeric series are described. Enantiomeric 4-O-silylated-4-hydroxymethyl-4-thiobutyrolactones, produced in high yield from chiral glycidols, provided suitable chiral synthons: phenylselenation of these intermediates resulted in anomeric selectivity in nucleobase glycosidations. L-d4-cytidine analogues showed marked anti-HBV and anti-HIV activity.

引用

页码：2599 / 2604

页数：6

共 27 条

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[2]

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