反应详情

A solution of 1-(4-Bromo-2-methyl-phenyl)-1-methyl-ethylamine (preparation 48, 544 mg, 2 mmol), vinyl sulfone (200 μl, 2 mmol) in EtOH (8 ml) is heated to 100° C. for 6 h and then allowed to cool to RT. EtOH is removed under HV and the residue is purified by flash chromatography (silicagel, CH2Cl2:EtOAc=1:0=>0:1) to afford the title compound as a pale pink solid, Rt=1.231 min (Acquity HPLC BEH C18, 2.1×50 mm, 1.7 micron, detection 215 nM, 0.1 min 2% CH3CN in H2O, 2% to 100% CH3CN in H2O in 1.5 min, 0.4 min 100% CH3CN+0.1% TFA, flow rate 1.0 ml/min); MS: 346 (M+1, 79Br)+.

1. customEtOH is removed under HV
2. customthe residue is purified by flash chromatography (silicagel, CH2Cl2:EtOAc=1:0=>0:1)