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

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概要

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• 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℃, 5kgf/cm^2 of H_2 pressure. The requisite Z-olefine was prepared regioselectively via coumarin derivative (5).

• 公益社団法人日本薬学会の論文
• 2000-10-01

著者

• Kobayashi Keijiro

  Process Development Laboratories Sankyo Co. Ltd.

• Hirai Koichi

  (present Address)research Institute Sankyo Co. Ltd.

• MURAKAMI Masayuki

  Process Development Laboratories, Sankyo Co., Ltd.

• Murakami Masayuki

  Process Development Laboratories Sankyo Co. Ltd.

関連論文

• 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

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