Sodium hydride → Pyrrole

Participants

Reaction Steps

Compound (V) is dissolved in a suspension of an ethereal or dipolar solvent, preferably in dry dimethylformamide, and mixed with sodium hydride. The mixture is heated to 45°-60° for 1-3 hours, preferably 2 hours. Suitable N-protecting agent R2, such as aroylchloride, alkanoylchloride, alkylchloroformate, preferably di-t-butylcarbonate, is added and the mixture is stirred at 60°-70° for 1-3 hours. After purification and crystallization of methods known in the art, ±1-R2 -protected-2-[phenethyl]-5-[3,4-methylenedioxy)benzoyl]pyrrole, preferably 1-t-butoxycarbonyl-2-[phenethyl]-5-[(3,4-methylenedioxy)benzoyl]pyrrole (VI) is obtained.

Provenance & Evidence