Development of a New Process for Tulobuterol Hydrochloride

Abstract Tulobuterol is a selective β2-adrenoceptor agonist and has been widely utilized as therapeutic agent for the treatment of asthma. Synthesis tulobuterol achieved many important progresses over past decades gradually become one research hotspots in organic chemistry. This study aimed to explore novel synthesis route synthesize hydrochloride (1), an active ingredient Chlobamolie Hydrochloride Tablets. In study, 1 was obtained from cost-effective, commercially available 2-chloroacetophenone through key steps including reactions bromination, NaBH4 reduction, amination. Process-related impurities were also investigated. with excellent purity (99.96%) 53% overall yield without need chromatographic purification. The developed method green, facile, cost-effective; thus, it suitable industrial-scale production 1.