反应详情

4-[5-(1-piperazinylmethyl)-1H-tetrazol-1-yl]-2-(trifluoromethyl)benzonitrile (Example 101, 50 mg, 0.15 mmol) was dissolved in DCM and treated with triethylamine (41 μL, 0.29 mmol) followed by 1-propanesulfonyl chloride (20 μL, 0.18 mmol). The mixture was stirred at ambient temperature under argon for 2.5 hours. The reaction mixture was partitioned between water and DCM (5 mL each) and the layers were separated using a hydrophobic frit. The aqueous layer was extracted with further DCM (2×5 mL). The combined DCM extracts were concentrated in vacuo to give the title compound as a pale cream solid (62 mg).

1. customThe reaction mixture was partitioned between water and DCM (5 mL each)
2. customthe layers were separated
3. extractionThe aqueous layer was extracted with further DCM (2×5 mL)
4. concentrationThe combined DCM extracts were concentrated in vacuo