FLUORODEHYDROXYLATION OF ANTHRACYCLINONES WITH DAST SYNTHESIS OF 8-(S)-FLUORODAUNORUBICIN

被引:13
作者
CANFARINI, F [1 ]
GIOLITTI, A [1 ]
GUIDI, A [1 ]
PASQUI, F [1 ]
PESTELLINI, V [1 ]
ARCAMONE, F [1 ]
机构
[1] A MENARINI IND FARMACEUT RIUNITE SRL, RIC CHIM LAB, VIA SETTE SANTI 3, I-50131 FLORENCE, ITALY
关键词
D O I
10.1016/S0040-4039(00)60660-3
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
8-(S)-fluoro-daunomycinone is obtained from daunomycinone in 5 synthetic steps and coupled with daunosamine to give, after two further deprotection steps, 8-(S)-fluorodaunorubicin, DAST [(diethylamino)sulfur trifluoride] accomplishes the fluorodehydroxylation reaction in the ring-A of a protected anthracyclinone with retention of configuration.
引用
收藏
页码:4697 / 4700
页数:4
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