Trifluoroacetic acid → Hexahydrocyclopenta(c)pyrrol-5(1H)-one

Participants

Reaction Steps

Reacting starting material 5-oxo-hexahydro-cyclopenta[c]pyrrole-2-carboxylic acid tert-butyl ester (I-1a) with trifluoroacetic acid in the solvent of dichloromethane in an ice-water bath to obtain hexahydro-cyclopenta[c]pyrrol-5-one triflutate (I-1b); reacting hexahydro-cyclopenta[c]pyrrol-5-one triflutate (I-1b) with acyl chloride or ester in the presence of base to give the compounds of formula (I-1c); reacting the compounds of formula (I-1c) with equivalent amounts of different amines, sodium triacetoxyborohydride and triethylamine in the solvent of methanol at room temperature to obtain the compounds of formula (IB).

Provenance & Evidence