SELECTIVE C-2 AND C-4 DEACYLATION AND ACYLATION OF TAXOL - THE FIRST SYNTHESIS OF A C-4 SUBSTITUTED TAXOL ANALOG

被引:28
作者
GEORG, GI [1 ]
ALI, SM [1 ]
BOGE, TC [1 ]
DATTA, A [1 ]
FALBORG, L [1 ]
HIMES, RH [1 ]
机构
[1] UNIV KANSAS,DEPT BIOCHEM,LAWRENCE,KS 66045
关键词
D O I
10.1016/0040-4039(94)88392-0
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Hydrolytic procedures for selective 2-debenzoylation and 2,4-dideacylation of 2'-0-tert-butyldimethylsilyl-7-0-(triethylsilyl)taxol are reported. The first synthesis and biological evaluation of a 4-substituted analogue, 4-deacetyl-4-isobutanoyltaxol, is presented. The chemistry described in this letter is suitable for the facile synthesis of taxol congeners modified at C-2 and/or C-4.
引用
收藏
页码:8931 / 8934
页数:4
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