反应详情

(S)-4-(2-chloro-6-neopentyl-6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidin-4-yl)-3-methylmorpholine (intermediate 7) (assumed 0.56 mmol) was stirred in CPME:EtOH:Water (7:3:2, freshly mixed, 2 mL) with 1-cyclopropyl-3-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)urea (203 mg, 0.67 mmol), Pd(PPh3)2Cl2 (20 mg, 0.028 mmol) and Na2CO3 (89 mg, 0.84 mmol) under a stream of nitrogen for 5 min, then irradiated in the microwave at 130° C. for 30 min. The reaction mixture was diluted with water and EtOAc and passed through a celite cartridge. The organic layer was concentrated in vacuo and purified by prep HPLC to give the desired compound as a yellow solid (48 mg, 0.103 mmol, 18% yield over three steps).

1. additionfreshly mixed
2. customirradiated in the microwave at 130° C. for 30 min
3. concentrationThe organic layer was concentrated in vacuo
4. custompurified by prep HPLC