2,2-Difluoro-2-(fluorosulfonyl)acetic acid → 6-chloro-3-(2-(difluoromethoxy)ethoxy)-4-methyl-1-trityl-1H-pyrazolo[4,3-c]pyridine

Participants

Reaction Steps

In a manner similar to that previously described (e.g. synthesis of Intermediate 59B/Step 2), 2-((6-chloro-4-methyl-1-trityl-1H-pyrazolo[4,3-c]pyridin-3-yl)oxy)ethanol was reacted with 2,2-difluoro-2-(fluorosulfonyl)acetic acid (copper(I) iodide, acetonitrile, 80° C. 30 min) to provide 6-chloro-3-(2-(difluoromethoxy)ethoxy)-4-methyl-1-trityl-1H-pyrazolo[4,3-c]pyridine 59% yield) as a white crystalline solid. MS: [M+H]+ m/z 520.

Provenance & Evidence