反应详情

温度

100 °C

(S)-ethyl 2-chloro-4-(3-methylmorpholino)-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate (intermediate 11) (1.0 g, 3.06 mmol), 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)aniline (805 mg, 3.67 mmol), Pd(PPh3)2(Cl)2 (107 mg, 0.15 mmol) and Na2CO3 (487 mg, 4.59 mmol) were stirred in CPME/Water/EtOH (14/1/6 mL) under nitrogen for 5 mins, followed by heating at 100° C. overnight. The reaction mixture was then diluted with water and CPME, and precipitate collected by filtration to give 1.05 g of a brown solid. A portion of the brown solid was further purified by prep. HPLC to give 32.6 mg of an off-white solid.

1. filtrationcollected by filtration