An efficient and stereoselective process for large scale synthesis of 3-(R)-3-(2,3-dihydrobenzofuran5-yl)-1,2,3,4-tetrahydropyrrolo[3,4-B]quinolin9-one

Li, Xun;Lemaire, Sébastien;Marko, Istvan;Willemsens, Albert
(2007)

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Authors
  • Li, XunJohnson & Johnson, New Brunswick
    Inventor
  • Lemaire, SébastienUCLouvain
    Inventor
  • Marko, IstvanUCLouvain
    Inventor
  • Willemsens, AlbertJohnson & Johnson, Beerse
    Inventor
Abstract
This invention relates to an efficient process for large scale stereose1ective production of (3R)-3-(2,3-dihydrobenzofuran-5-yl)-1 ,2,3,4-tetrahydropyrrolo[3,4-B]quinolin-9-ones and key intennediates used for the preparation of benzofuranyl pyrroloquinolones as potent and selective PDE5 inhibitors for the treatment of erectile dysfunction, as weil as pharmaceutical compositions and methods of treatment utilizing these compounds.
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Li, X., Lemaire, S., Marko, I., & Willemsens, A. (2007). An efficient and stereoselective process for large scale synthesis of 3-(R)-3-(2,3-dihydrobenzofuran5-yl)-1,2,3,4-tetrahydropyrrolo[3,4-B]quinolin9-one (Patent No. WO 2006093719 A1). https://hdl.handle.net/2078.5/26443