4-Methylmorpholine → HCID 57988757, compound

Participants

Reaction Steps

A mixture of 3-(3-{4-[2,6-dioxo-1,3-dipropyl-7-(2-trimethylsilanyl-ethoxymethyl)-2,3,6,7-tetrahydro-1H-purin-8-yl]-pyrazol-1-yl}-prop-1-ynyl)-benzoic acid (100 mg, 0.17 mmol), ammonium carbonate (33 mg, 0.34 mmol), HOBT (36 mg, 0.24 mmol), N-methyl morpholine (34 mg, 0.34 mmol) were taken in DMF (2 ml), EDCI (130 mg, 0.68 mmol) was added at cold condition and stirred for 18 hrs at room temperature. The reaction mixture was diluted with water (10 ml) and extracted with DCM (3×5 ml), the organic layer was washed with brine (2×10 ml), dried over Na2SO4. The organic solvent was evaporated and the crude product was purified using HPLC to obtain 3-(3-{4-[2,6-Dioxo-1,3-dipropyl-7-(2-trimethylsilanyl-ethoxymethyl)-2,3,6,7-tetrahydro-1H-purin-8-yl]-pyrazol-1-yl}-prop-1-ynyl)-benzamide (33 mg, 18%).

Provenance & Evidence