Potassium Carbonate → 1-Benzyl-2'-(4-phenoxyphenyl)-5',7'-dihydro-4'H-spiro[azetidine-3,6'-pyrazolo[1,5-a]pyrimidine]-3'-carbonitrile

Participants

Reaction Conditions

Reaction Steps

To a solution of (1-benzylazetidine-3,3-diyl)bis(methylene)dimethanesulfonate (300 mg, 0.83 mmol) in DMF (10 mL) was added 5-amino-3-(4-phenoxyphenyl)-1H-pyrazole-4-carbonitrile (230 mg, 0.83 mmol) and K2CO3 (230 mg, 1.66 mmol). The mixture was stirred at 80° C. under N2 for 16 hr. The mixture was concentrated. The residue was washed with H2O (100 mL×2), dried and purified by pre-TLC (DCM/CH3OH=10/1) to afford 30 mg (10%) of desired product as a yellow liquid. MS (ESI) m/e [M+1]+ 447.9.

Provenance & Evidence