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Paper | Regular issue | Vol 43, No. 8, 1996, pp.1719-1734
Published online, 1st January, 1970
DOI: 10.3987/COM-96-7505
A Convenient Synthesis of N-Substituted 2,3-Dihydro-3-oxoisothiazolo[5,4-b]pyridines in Acidic Condition

Hideo Terauchi,* Akihiko Tanitame, Keiko Tada, and Yoshinori Nishikawa

*Discovery Research Laboratories Ö†, Dainippon Pharmaceutical Co., Ltd., Enoki 33-94, Suita, Osaka 564, Japan

Abstract

A novel and convenient synthesis of N-substituted 2,3-dihydro-3-oxoisothiazolo[5,4-b]pyridines which possess potent in vitro inhibitory activity against gastric (H+/K+)-ATPase is reported. Compared with the methods reported previously, the compounds were syntehsized more readily in relatively high yields by conversion of N-substituted 2-(benzyl-, 1-phenylethyl-, and benzhydrylsulfinyl)nictinamides (17d-l) in a diluted hydrochloricccc acid-methanol solution at room tempeature.