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.
Notes
a According to 1H NMR analysis.
b Conditions directly switched to LiCl/DMF; DMF alone was not tested.
a According to GC and TLC analysis.