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Synlett 1997; 1997(12): 1472-1474
DOI: 10.1055/s-1997-1079
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An Efficient Method for the Synthesis of a Novel Leukotriene B4 Receptor Antagonist, ONO-4057, via Michael Reaction of Dihydroresorcinol

Mitoshi Konno, Takahiko Nakae, Shigeru Sakuyama, Katsuhiro Imaki, Hisao Nakai, Nobuyuki Hamanaka*
  • *Department of Medicinal Chemistry, Minase Research Institute, Ono Pharmaceutical Co., Ltd., Shimamoto, Mishima, Osaka 618, Japan, Fax +81-75-962-9314
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Publication Date:
31 December 2000 (online)

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A practical method for the synthesis of ONO-4057, a highly potent and orally active leukotriene B4 (LTB4) receptor antagonist, was developed. This method includes improved synthesis of a key intermediate, 1,3-dioxo-2-(2-ethoxycarbonylethyl)cyclohexane (6).

leukotriene B4 - antagonist - dihydroresorcinol - Michael addition