Benzyl hexahydropyrrolo[3,4-c]pyrrole-2(1H)-carboxylate → Benzyl 5-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(4-cyanophenoxy)-propyl]hexahydropyrrolo[3,4-c]pyrrole-2(1H)-carboxylate

Participants

Reaction Conditions

Reaction Steps

tert-Butyl (2S)-2-[(4-cyanophenoxy)methyl]aziridine-1-carboxylate (2.5 g, 9.1 mmol; see step (f) above) and benzyl hexahydropyrrolo[3,4-c]pyrrole-2(1H)-carboxylate (2.24 g, 9.1 mmol; see step (h) above) was dissolved in isopropanol (30 mL) and was stirred at 56° C. for 24 h. The solvent was then evaporated. The product was purified by chromatography on silica (ethyl acetate, 0–5% MeOH eluant), giving 3.8 g (80%) of the sub-title compound.

Provenance & Evidence