A novel and practical route to A-ring enyne synthon for 1α,25-dihydroxyvitamin D3 analogs:: Synthesis of A-Ring diastereomers of 1α,25-dihydroxyvitamin D3 AND 2-methyl-1,25-dihydroxyvitamin D3

被引：83

作者：

Konno, K

Maki, S

Fujishima, T

Liu, ZP

Miura, D

Chokki, M

Takayama, H ^{[1
]}

机构：

[1] Teikyo Univ, Fac Pharmaceut Sci, Kanagawa 19901, Japan

[2] Teijin Ltd, Biomed Res Inst, Tokyo 191, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(97)10204-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel and practical route to the A-ring enyne synthon (2), which can be versatile for a variety of A-ring analogs of 1 alpha,25-dihydroxyvitamin D-3 (1), was developed. This novel method led to an improved synthesis of the A-ring diastereomers of 1, the compounds 13-15, and synthesis of the new analogs, 2-methyl-1,25-dihydroxyvitamin D-3 (4) with its all possible diastereomers. The biological evaluation of the 2-methyl analogs showed the alpha alpha beta-isomer to be more potent than 1. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：151 / 156

页数：6

共 26 条

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