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Synlett 1992; 1992(6): 531-533
DOI: 10.1055/s-1992-21405
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Synthesis of a Novel Serotonin-3 (5-HT3) Receptor Antagonist

Tsuneyuki Sugiura* , Toshiaki Matsui, Hisao Nakai, Masaki Okamoto, Shinsuke Hashimoto, Yoichi Iguchi, Hirohisa Wakatsuka, Masanori Kawamura
  • *Minase Research Institute, Ono Pharmaceutical Co., Ltd., Shimamoto Mishima, Osaka 618, Japan
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Publication Date:
08 March 2002 (online)

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A practical method for the synthesis of ONO-3051 {6-amino-7-chloro-2-[(5-methyl-4-imidazolyl)methyl]isoquinolin-1-(2H)-one (3)}, a highly potent and orally active serotonin-3 (5-HT3) receptor antagonist, was developed. This method includes an efficient synthesis of a key intermediate, 6-amino-7-chloroisoquinolin-1(2H)-one (10).