Kooji KAGARA*, Shunsuke GOTO** and Masaharu ICHIHARA** Vamicamide is a new anticholinergic agent useful for the treatment of urinary incontinence . Vamicamide is synthesized from benzonitrile in 6 steps which include reductive amination and separation of diastereomers as key steps. In this paper, the process development of Vamicamide is described not only from the point of organic synthesis but also from the industrialization standpoints such as scale-up, economy, safety and environmental control.