Ethyl 3-(1-{[(tert-butoxy)carbonyl]amino}cyclopropyl)-3-oxopropanoate → ethyl 2-(1-((tert-butoxycarbonyl)amino)cyclopropyl)-5-(3-((2,2-difluoroethyl)amino)-2-methylquinoxalin-5-yl)-1H-pyrrole-3-carboxylate

Participants

Reaction Steps

This compound (0.40 g, 41% yield) as a yellow amorphous solid was prepared according to the procedures described for Intermediate 324b, using 2-bromo-1-(34(2,2-difluoroethyl)amino)-2-methylquinoxalin-5-yl)ethanone (617) (583 mg, 2.26 mmol), ethyl 3-(1-((tert-butoxycarbonyl)amino)cyclopropyl)-3-oxopropanoate (604) (650 mg, 1.89 mmol) as the starting materials, followed by the subsequent treatment of the resulting 331a (m/z (ESI, +ve) 535.2 (M+H)+) with NH4OAc (728 mg, 9.44 mmol) in 3 mL of EtOH and 1.5 mL of HOAc at 50° C. for 4 h. m/z (ESI, +ve) 516.2 (M+H)+.

Provenance & Evidence