Cl[CH2:2][C:3]([NH:5][CH2:6][C:7]1([CH3:12])[CH2:11][CH2:10][CH2:9][NH:8]1)=[O:4].C([O-])([O-])=O.[K+].[K+].[Na+].[I-]>CC#N.O>[CH3:12][C:7]12[CH2:11][CH2:10][CH2:9][N:8]1[CH2:2][C:3](=[O:4])[NH:5][CH2:6]2A solution of 2-chloro-N-((2-methylpyrrolidin-2-yl)methyl)acetamide (˜300 mg), K2CO3 (1.0 g, 7.2 mmol) and a catalytic amount of NaI in CH3CN was stirred at 80° C. for about 3 h. The reaction was monitored by LC-MS. After cooling to room temperature, the suspension was diluted with water (30 mL) and extracted with DCM (8×100 mL). Then the combined organic layers were concentrated to give 120 mg of the desired product, which was directly used for the next step without further purification. MS (ESI): 155 (MH+).
Loading…
