Tetrahedron

Process development of potassium channel opener, TCV-295, based on convenient ring formation of 2H-1, 3-benzoxazine and selective N-oxidation of the pyridyl …

H Mizufune, H Irie, S Katsube, T Okada, Y Mizuno…

Index: Mizufune, Hideya; Irie, Hiroyuki; Katsube, Susumu; Okada, Tadataka; Mizuno, Yukio; Arita, Miichiro Tetrahedron, 2001 , vol. 57, # 35 p. 7501 - 7506

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Citation Number: 6

Abstract

An efficient process for potassium channel opener, TCV-295, based on a novel and convenient 4-(2-pyridyl)-2H-1, 3-benzoxazine ring formation from o-hydroxybenzoylpyridine by the NH4I/piperidine/2, 2-dimethoxypropane system and the following selective pyridine-N- oxidation using dimethyldioxirane, has been developed. Additionally, the combination reagent of ammonium halide and sec-or tert-amine conveniently converted o- ...