Methyl iodide → (+/-)-(5S,7aR)-7-(2,5-Difluorophenyl)-2-methyl-5-phenyl-1,2,5,7a-tetrahydro-3H-pyrrolo[1,2-c]imidazol-3-one

Participants

Reaction Steps

A solution of 2-4a (0.02 g, 0.06 mmol), sodium hydride (5 mg), and iodomethane (0.004 mL, 0.03 mmol) in THF (1.0 mL) was stirred at rt for 1 h. The reaction was quenched with water (2.0 mL) and extracted with EtOAc (20 mL). The organic solution was washed with brine, dried over MgSO4, filtered, and concentrated. The remaining oil was dissolved in CH3CN (0.5 mL) and purified on a Gilson automated system affixed with a YMC J'sphere H80 20×50 mm column (eluting with 5-95% CH3CN +0.1% TFA in water +0.1% TFA over 10 min) to afford pure 2A-1a.

Provenance & Evidence