反应详情

Prepared according to procedure N using tert-butyl 6′-bromo-2,3,5,6-tetrahydrospiro[pyran-4,3′-pyrrolo[3,2-b]pyridine]-1′(2′H)-carboxylate (12.0 g, 32.5 mmol), morpholine (3.11 mL, 35.7 mmol), Pd2dba3 (1.19 g, 1.30 mmol), XPhos (1.24 g, 0.08 mmol) and sodium tert-butoxide (6.25 g, 65.0 mmol) in toluene (200 mL) at 110° C. for 5 h. Purification by column chromatography (hexanes:EtOAC, 1:0 to 1:3 as eluent) gave tert-butyl 6′-morpholino-2,3,5,6-tetrahydrospiro[pyran-4,3′-pyrrolo[3,2-b]pyridine]-1′(2′H)-carboxylate. Mass Spectrum (ESI) m/e=376.2 (M+1).

1. customPrepared
2. customat 110° C.
3. customfor 5 h
4. customPurification by column chromatography (hexanes:EtOAC, 1:0 to 1:3 as eluent)