Phthalimide → HCID 66780004, compound

Participants

Reaction Steps

DEAD (0.035 mL, 0.221 mmol) was added to a solution of 5-(hydroxymethyl)-4-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-2-(4-morpholinyl)[1,3]thiazolo[4,5-d]pyrimidin-7(4H)-one (Example 113, 65 mg, 0.148 mmol), 1H-isoindole-1,3(2H)-dione (26.1 mg, 0.177 mmol) and triphenylphosphine (58.1 mg, 0.221 mmol) in Tetrahydrofuran (THF) (2 mL). The reaction was stirred at RT for overnight. The mixture was partitioned between DCM and NaCl solution, the organic layer was dried over MgSO4 and was concentrated. The residue was purified on a silica column eluting with 30% EtOAc/Hexanes to give the titled product, 60 mg (60%).

Provenance & Evidence