反应详情

To a solution of (3S,4R)-3-amino-4-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)pyrrolidine-1-carboxylate (2.1 g, 4.1 mmol) in dichloromethane (82 mL) at 0° C. was added DIEA (1.07 mL, 6.1 mmol) and acryloyl chloride (0.36 mL, 4.5 mmol) and the reaction was stirred for 30 mins. LC-MS indicated complete consumption of SM. The reaction mixture was purified by silica gel chromatography to yield tert-butyl (3S,4R)-3-acrylamido-4-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)pyrrolidine-1-carboxylate (1.26 g, 52%). MS (ES+) C28H31Cl2N5O5 requires: 587, found: 588.

1. customconsumption of SM
2. customThe reaction mixture was purified by silica gel chromatography