3,5-di-(tert-butyl)-6-fluoro-cycloSal-d4TMP -: A pronucleotide with a considerably improved masking group

被引：14

作者：

Ducho, C

Wendicke, S

Görbig, U

Balzarini, J

Meier, C

机构：

[1] Univ Hamburg, Inst Organ Chem, D-20146 Hamburg, Germany

[2] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium

来源：

EUROPEAN JOURNAL OF ORGANIC CHEMISTRY | 2003年 / 2003卷 / 24期

关键词：

antiviral agents; DNA; nucleosides;

D O I：

10.1002/ejoc.200300537

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A new, considerably improved cycloSal masking group has been developed. This new group combines four desirable properties and has been attached to the anti-HIV drug 2',3'-dideoxy-2',3'-didehydrothymidine (d4T, 1) to give 3,5-(di-tert-butyl)-6-fluoro-cycloSal-d4TMP (2i). This phosphate triester has a reasonable chemical half-life, highly selectively released d4TMP, has poor - if any - inhibitory effect on butyrylcholinesterase (BChE), and achieved the TK-bypass. ((C) Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003)

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页码：4786 / 4791

页数：6

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