4-Methylmorpholine → 4-(5-{[(2S)-2-(Trifluoromethyl)-1-pyrrolidinyl]methyl}-1H-tetrazol-1-yl)benzonitrile

Participants

Reaction Conditions

Reaction Steps

To a mixture of 4-[5-(chloromethyl)-1H-tetrazol-1-yl]benzonitrile (100 mg, 0.455 mmol, Intermediate 10) and polymer supported N-methylmorpholine (4 mmol/g, 171 mg, 0.683 mmol) in acetonitrile (3 mL) was added (2S)-2-(trifluoromethyl)pyrrolidine (95 mg, 0.683 mmol). The reaction mixture was heated at 120° C. for 20 min in a microwave reactor and at 140° C. for 20 min and at 150° C. for 30 min and finally at 160° C. for 30 min in the microwave reactor.

Provenance & Evidence