Alternative synthesis of bilastine

SJ Collier, X Wu, Z Poh, GA Rajkumar…

Index: Collier, Steven J.; Wu, Xiang; Poh, Zhiying; Rajkumar, Gurubatham Abraham; Yet, Larry Synthetic Communications, 2011 , vol. 41, # 9 p. 1394 - 1402

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Citation Number: 3

Abstract

Abstract A new and efficient synthesis of the non-sedating histamine H1 receptor antagonist Bilastine is reported. The new route employs a convergent strategy, with a longest linear sequence of five steps, giving slightly improved yields over the previous routes. The use of anhydrous metal-halogen exchange, hazardous ethylene oxide, and a tedious protection of the carboxylic acid function are all avoided.