Hydrochloric Acid → Hydrochloric Acid

Participants

Reaction Steps

To tert-butyl (2R,6S,13aS,14aR,16aS)-14a-(cyclopropylsulfonylcarbamoyl)-12,12-difluoro-5,16-dioxo-2-(quinoxalin-2-yloxy)octadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-6-ylcarbamate (Example 1, 8.81 mg, 0.012 mmol) was added ethyl acetate (60 μl) followed by HCl (4 N in dioxane, 60 μl, 0.240 mmol). The solution was stirred at room temperature for 4 hr (a solid appeared), and LC/MS showed completion. The reaction mixture was concentrated to give the title compound (2R,6S,13aS,14aR,16aS)-6-amino-N-(cyclopropylsulfonyl)-12,12-difluoro-5,16-dioxo-2-(quinoxalin-2-yloxy)octadecahydrocyclo propa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a-carboxamide, hydrochloric acid (8.05 mg, quantitative yield).

Provenance & Evidence