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 …
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- ...