A VERSATILE SYNTHESIS OF 2-METHOXYESTRADIOL, AN ENDOGENOUS METABOLITE OF ESTRADIOL WHICH INHIBITS TUBULIN POLYMERIZATION BY BINDING TO THE COLCHICINE BINDING-SITE

被引：16

作者：

HE, HM ^{[1
]}

CUSHMAN, M ^{[1
]}

机构：

[1] PURDUE UNIV,DEPT MED CHEM & PHARMACOGNOSY,W LAFAYETTE,IN 47907

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(00)80369-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A versatile synthesis of 2-methoxyestradiol (7) is described. Formylation of estradiol (1) with hexamethylenetetramine gave 2-formylestradiol (3). Benzylation of the two hydroxyl groups of 3 under basic conditions with benzyl bromide afforded the dibenzyl ether 4. 2-Methoxyestradiol (7) was then obtained from 4 by Baeyer-Villiger oxidation, methylation of the phenol, and debenzylaion.

引用

页码：1725 / 1728

页数：4

共 14 条

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