反应详情

A mixture of 5-chloro-4-(cyclobutyl(hydrazono)methyl)-1H-pyrrolo[2,3-b]pyridine (0.052 g, 0.21 mmol), sodium tert-butoxide (0.048 g, 0.50 mmol), palladium acetate (0.0005 g, 0.0025 mmol) and (R)-1-[(S)-2-(dicyclohexylphosphino)ferrocenyl]ethyl di-tert-butyl phosphine (0.0015 g, 0.0025 mmol) was heated in N-methyl-2-pyrrolidinone (2 mL) at about 160° C. in a CEM Discover microwave for about 30 min. The insoluble residue was removed by filtration and the filtrate was subjected to purification by preparative RP-HPLC (Table 2, Method h) to yield 1-cyclobutyl-3,6-dihydropyrazolo[4,3-d]pyrrolo[2,3-b]pyridine as a white solid (0.002 g, 4%): LC/MS (Table 2, Method d) Rt=1.78 min; m/z: 213 (M+H)+.

1. customThe insoluble residue was removed by filtration
2. customthe filtrate was subjected to purification by preparative RP-HPLC (Table 2, Method h)