Formaldehyde → HCID 118060296, compound

Participants

Reaction Steps

To a solution of 6-fluoro-1-(phenylsulfonyl)-3-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)-1H-indole hydrochloride (Intermediate 17; 290 mg), Et3N (55 mg; 0.55 mmol)cOH (1 drop), and 37% aqueous HCHO (89 mg; 1.1 mmol) in MeOH (10 mL) was added NaBH(OAc)3 (233 mg; 1.05 mmol). The reaction mixture was stirred for 16 h and concentrated. The residue was dissolved in DCM (20 mL) and washed with saturated NaHCO3 (20 mL). The organic layer was dried over anhydrous Na2SO4, filtered, and concentrated to afford 270 mg (>100%) of the title compound as a white solid.

Provenance & Evidence