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

Masayuki MURAKAMI; Keijiro KOBAYASHI; Koichi HIRAI

doi:10.1248/cpb.48.1567

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

Masayuki MURAKAMI, Keijiro KOBAYASHI, Koichi HIRAI

著者情報

キーワード: enantioselective hydrogenation, (R)-BINAP-Ru(OAc)₂, coumarin derivative, ACAT inhibitor

ジャーナルフリー

2000 年 48 巻 10 号 p. 1567-1569

DOI https://doi.org/10.1248/cpb.48.1567

詳細

抄録

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

責任著者(Corresponding author)

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