Enantioselective synthesis of the key intermediate of the acyl-CoA:: Cholesterol acyltransferase (ACAT) inhibitor (R-106578) using 2,2′-bis(diphenylphosphino)-1,1'-binaphthyl (BINAP)-Ru(OAc)2 as a catalyst

被引:0
|
作者
Murakami, M [1 ]
Kobayashi, K [1 ]
Hirai, K [1 ]
机构
[1] Sankyo Co Ltd, Proc Dev Labs, Hiratsuka, Kanagawa 2548560, Japan
关键词
enantioselective hydrogenation; (R)-BINAP-Ru(OAc)(2); coumarin derivative; ACAT inhibitor;
D O I
暂无
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Acidic segment of an acyl-CoA: cholesterol acyltransferase (ACAT) inhibitor, R-106578 was synthesized by enantioselective hydrogenation of the Z-olefine (9-(Z)) using (R)-2,2'-bis(diphenylphosphino)-1,1'-binaphthyl (BINAP)-Ru(OAc)(2) as a catalyst in methanol at 100 degrees C, 5 kgf/cm(2) of H-2 pressure. The requisite Z-olefine was prepared regioselectively via coumarin derivative (5).
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页码:1567 / 1569
页数:3
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