Cesium carbonate → HCID 71473972, compound

Participants

Reaction Steps

4-((1R,2R)-2-(((2-fluoro-4-(methylsulfonyl)benzyl)oxy)methyl)cyclopropyl)piperidine hydrochloride (Step D product) was dissolved in DMSO (7 ml) at RT under N2 and Cs2CO3 (539 mg, 1.654 mmol) was added. The mixture was stirred at RT for 5 min and chloropyrimidine aldehyde (113 mg, 0.794 mmol) in DMSO (1 mL) was added. The mixture was stirred at RT overnight. The mixture was diluted with EtOAc, washed with sat. NH4Cl, dried over MgSO4, evaporated to dryness. The crude material was purified by flash column (25 g SNAP, 25˜60% EtOAc in hexane) to afford 200 mg of the desired product (67.6%) as a white solid. LC/MS (m/z): 448 (M+H)+.

Provenance & Evidence