Morpholine → HCID 21084072, compound

Participants

Reaction Steps

To a mixture of the compound of Example 57 (100 mg, 0.22 mmol), caesium carbonate (101 mg, 0.31 mmol), Pd(OAc)2 (5 mg, 0.022 mmol, 10 mol %) and 2,2′-bis(diphenylphosphino)-1-1′-binaphthyl (BINAP) (21 mg, 0.033 mmol, 15 mol %) in toluene (2 mL) and under nitrogen was added morpholine (0.024 mL, 0.27 mmol). The reaction mixture was heated to 100° for 18 h. Solvent was removed in vacuo and the crude product purified by chromatography on silica (0–20% THF in DCM) to give the title compound as a white solid (40 mg).

Provenance & Evidence