Boron tribromide → HCID 57554982, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of 99 mg (0.22 mmol) [3-methoxymethyl-5-methyl-1-(3-trifluoromethyl-phenyl)-1H-pyrazol-4-yl]-(4-pyrrolidin-1-yl-piperidin-1-yl)-methanone (Example 155D]) in 1.8 ml of CH2Cl2 was treated at −30° C. with 0.28 ml BBr3 (1M in dichloromethane, 0.28 mmol). The reaction was warmed up (0° C. for 1 h) and stirred 1.5 h at 0° C. The reaction was treated with saturated NaHCO3-solution. The mixture was extracted with EtOAc (3×), the organic phase was washed with a NaCl solution (10%), dried (Na2SO4) and evaporated. The crude product was purified by flash chromatography over silica gel with CH2Cl2/MeOH 2.5% to 10%, to give 18 mg (19%) of the title compound as light yellow foam. MS: 437.3 (MH+).

Provenance & Evidence