Methanol → Estradiol diacetate

Participants

Reaction Steps

Under an N2-atmosphere, Ac2O (375 ml, 3.993 mol) was added dropwise during 20 min to a solution of estradiol (150 g, 0.551 mol) in pyridine (1500 ml). The clear colorless solution obtained was stirred at RT overnight. The reaction mixture was then cooled to 0° C. and MeOH (375 ml) was added dropwise during 25 min. The reaction mixture was stirred at 0° C. for 2 h, then allowed to warm to RT and concentrated in vacuo. The residue was recrystallized from hot MeOH to yield (C2-2) (176 g, 90%) as white crystals.

Provenance & Evidence