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.

Abstract:

: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/cm2 of H2 pressure. The requisite Z-olefine was prepared regioselectively via coumarin derivative (5).

authors

Murakami M,Kobayashi K,Hirai K

doi

10.1248/cpb.48.1567

subject

Has Abstract

pub_date

2000-10-01 00:00:00

pages

1567-9

issue

10

eissn

0009-2363

issn

1347-5223

journal_volume

48

pub_type

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