HCID 57941342, compound → HCID 57941494, compound

Participants

Reaction Steps

A solution of (4R,7S)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-4,7-methano-indazol-3-one (Intermediate 48; 250 mg, 1.2 mmol) and 4-bromomethyl-3-trifluoromethyl-1-trityl-1H-pyrazole (Intermediate 2; 580 mg, 1.2 mmol) in dimethylformamide (12 mL) was heated at 100° C. for 4.5 h. The solvent was evaporated and the residue was purified on a Biotage 40S chromatography system, eluting with 0-3% methanol/dichloromethane. Fractions homogeneous for the product were concentrated and the residue held under high vacuum to give (4R,7S)-1,7,8,8-tetramethyl-2-(3-trifluoromethyl-1-trityl-1H-pyrazol-4-ylmethyl)-1,2,4,5,6,7-hexahydro-4,7-methano-indazol-3-one (420 mg, 58%) as a viscous golden orange oil.

Provenance & Evidence