MANIPULATION OF THE RAPAMYCIN EFFECTOR DOMAIN - SELECTIVE NUCLEOPHILIC-SUBSTITUTION OF THE C-7 METHOXY GROUP

被引：19

作者：

LUENGO, JI

KONIALIANBECK, A

ROZAMUS, LW

HOLT, DA

机构：

[1] Department of Medicinal Chemistry, SmithKline Beecham Pharmaceuticals, Pennsylvania 19406, P. O. Box 1539, King of Prussia

来源：

JOURNAL OF ORGANIC CHEMISTRY | 1994年 / 59卷 / 22期

关键词：

D O I：

10.1021/jo00101a006

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The C-7 methoxy group in rapamycin has been found to be labile toward acidic reagents. Conditions have been developed to replace this group with a number of different nucleophiles, such as alcohols, thiols, and electron-rich aromatic systems. This novel, efficient transformation allows the selective manipulation of the rapamycin effector domain.

引用

页码：6512 / 6513

页数：2

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