Citric Acid → HCID 75277248, compound

Participants

Reaction Steps

Compound 1i (78 mg, 0.146 mmol) and EDAC (34 mg, 0.175 mmol) were dissolved in DCM (3 ml). The reaction mixture was stirred at room temperature for 1 h (LC-MS indicated presence of the intermediate). Cyclopropane sulphonic amide (20 mg, 0.161 mmol) and DBU (46 μl, 0.307 mmol) were added and the reaction mixture was stirred at RT for 3.5 h. Citric acid (5%) was added and the organic layer was separated and washed with brine, dried (MgSO4), filtered and evaporated. The residue was purified by preparative HPLC which gave the pure title compound (50 mg, 54%), (M+H)+639).

Provenance & Evidence