Trifluoroacetic acid → 3-Methoxy-pyrrolidine-3-carboxylic acid [3-(2-methoxy-pyridin-4-yl)-1H-indazol-5-yl]-amide

Participants

Reaction Steps

To the stirred solution 3-Methoxy-3-[3-(2-methoxy-pyridin-4-yl)-1-trityl-1H-indazol-5-ylcarbamoyl]-pyrrolidine-1-carboxylic acid tert-butyl ester 7BV (2.95 g, 4.16 mmole) in DCM (50 mL) at r.t. was added triethylsilane (1.00 ml, 6.24 mmole) followed by TFA (10 mL). The mixture was stirred at r.t. under dry N2 gas for 4-5 hours. The mixture was evaporated to dryness and co-evaporated with dry toluene (2×75 mL). The resulting crude solid was purified on RediSep 120 g cartridge eluting with 2.5%-6% 2M NH3-MeOH/CH2Cl2 to yield an off-white solid 8BV (1.23 g, 80%).

Provenance & Evidence