Methylamine → HCID 89438439, compound

Participants

Reaction Steps

The intermediate from Step A above (35 mg, 0.058 mmol), methylamine (0.058 mL, 0.117 mmol, 2M in THF) and THF (0.5 mL) were stirred in a sealed tube at 50° C. for 1.5 h, then at 65° C. overnight. The reaction mixture was subjected to microwave irradiation at 150° C. for 2 h, The reaction mixture was partitioned between brine and EtOAc. The combined organic extracts were dried (Na2SO4), filtered and concentrated in vacuo. The residue was purified by reverse phase HPLC to afford the indicated product, as a solid. 1H NMR (500 MHz, CD3OD): δ 8.64 (d, J=8.7 Hz, 1H); 7.77 (d, J=1.6 Hz, 1H); 7.38-7.31 (m, 4H); 7.32-7.28 (m, 2H); 4.82 (d, 7.1 Hz, 2H); 3.07 (s, 3H); 3.00-2.88 (m, 2H); 1.88 (s, 3H). m/z=551.0 (WE).

Provenance & Evidence