Water → HCID 67444143, compound

Participants

Reaction Steps

To a stirred suspension of 271 (150 mg, 0.302 mmol) and DIPEA (123 μL, 0.707 mmol) in DMF (10 mL) was added methyl succinyl chloride (65 μl, 0.53 mmol). The reaction mixture was stirred at RT for 2.5 days. Water was added and the reaction mixture was extracted with DCM. The organic layer was successively washed with brine, dried over anhydrous sodium sulfate, filtered and concentrated. The residue was purified by Biotage (SNAP 80 g cartridge; MeOH/DCM: 0/100 to 10/90 over 20 CV), to afford the title compound 272 (120 mg, 0.223 mmol, 63% yield) as an off-white solid. MS (m/z): 539.5 (M+H).

Provenance & Evidence