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.
![tert-Butyl 4-(1H-benzo[d]imidazol-2-yl)piperidine-1-carboxylate Structure](https://image.chemsrc.com/caspic/032/953071-73-3.png)
