Dichloromethane → HCID 53497470, compound

Participants

Reaction Steps

2-(3-(4-(7-(1-Methyl-1H-pyrazol-4-yl)imidazo[1,2-c]pyrimidin-5-yl)-1H-pyrazol-1-yl)azetidin-3-yl)acetonitrile hydrochloride (Example 62; 7.1 mg, 0.016 mmol) was suspended in DCM (90 μL, 0.018 mmol) and cooled in an ice bath. To this was added triethylamine (7.5 μL, 0.054 mmol) followed by propane-2-sulfonyl chloride (2.7 mg, 0.019 mmol). The reaction mixture was allowed to warm to ambient temperature. After 15 hours, the reaction mixture was diluted in EtOAc and washed with water and brine. The organic layer was dried with MgSO4, filtered and concentrated down to afford 2-(1-(isopropylsulfonyl)-3-(4-(7-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-c]pyrimidin-5-yl)-1H-pyrazol-1-yl)azetidin-3-yl)acetonitrile (4.8 mg, 0.010 mmol, 58% yield) as a light yellow oil. MS (apci) m/z=466.6 (M+H).

Provenance & Evidence