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：82
|
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.
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收藏
页码：151 / 156
页数：6
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