Diisopropylethylamine → {5-tert-Butyl-2-[1-(2-morpholin-4-yl-ethyl)-1H-indazol-6-yl]-2H-pyrazol-3-yl}-carbamic acid 2,2,2-trichloro-ethyl ester

Participants

Reaction Steps

A solution of Intermediate 24a (134 mg, 0.36 mmol) was formed in THF (10 mL). DIPEA (125 μL, 0.72 mmol) was added followed by the dropwise addition of a solution of 2,2,2-trichloroethylchloroformate (50 μ□L, 0.36 mmol) in THF (2 mL). The mixture was stirred at RT for 4 h, then partitioned between EtOAc/water and extracted with EtOAc. The combined organics were dried over Na2SO4, filtered and concentrated in vacuo. Purification by FCC, using 0-10% MeOH in EtOAc, gave the title compound (200 mg, 99%) as a colourless film. LCMS (Method 4): Rt 2.59, m/z 543, 545 [MH+].

Provenance & Evidence