Synthetic approaches to a mononucleotide prodrug of cytarabine

被引：19

作者：

Bazzanini, R

Gouy, MH

Peyrottes, S

Gosselin, G

Périgaud, C

Manfredini, S

机构：

[1] Univ Montpellier 2, CNRS, UMR 5625, Montpellier, France

[2] Univ Ferrara, Dipartimento Sci Farmaceut, Ferrara, Italy

来源：

NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS | 2005年 / 24卷 / 10-12期

关键词：

Ara-C; leukemia; prodrug; phosphotriester;

D O I：

10.1080/15257770500267006

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Synthetic pathways to a mononucleotide prodrug of cytarabine (Ara-C) bearing S-pivaloyl-2-thioethyl (tBuSATE) groups, as biolabile phosphate protections, are reported. Using a common phosphoramidite approach, two different kinds of nucleoside protecting groups have been investigated. During this study, we observed an intermolecular migration of the Boc protecting group in the course of the tert-butyldimethylsilyl ether cleavage using tetrabutyl ammonium fluoride.

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收藏

页码：1635 / 1649

页数：15

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