Cesium carbonate → HCID 86686017, compound

Participants

Reaction Steps

A mixture of 5-chloro-3,3-dimethyl-2,3-dihydro-isoindol-1-one (intermediate A-12, 160 mg, 0.82 mmol), 1-[3-(5-bromo-pyridin-3-yl)-pyrrolidin-1-yl]-ethanone (160 mg, 0.6 mmol), CuI (34 mg, 0.8 mmol), (1S,2S)-cyclohexane-1,2-diamine (41 mg, 0.36 mmol) and Cs2CO3 (390 mg, 1.2 mmol) were dissolved in dioxane (5 mL). The reaction mixture was subjected to microwave reaction at 150° C. for 2.5 hours before it was poured into H2O (50 mL) and extracted with EtOAc (25 mL×2). The combined organic layers were washed with brine, dried over anhy. Na2SO4, filtered and concentrated in vacuo to give a crude product which was then purified by Prep-HPLC to yield the title compound (23 mg, 10%) as a white solid. MS: 384.2 (M+H+).

Provenance & Evidence