Methylamine → HCID 86679015, compound

Participants

Reaction Steps

The intermediate from Step A above (100 mg, 0.176 mmol), methylamine (0.881 mL, 1.763 mmo, 2 M in THF) and THF (2 mL) were sealed in a microwave tube and subject to microwave irradiation at 140° 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 give the title product, as a solid. 1H NMR (500 MHz, CD3OD) δ 9.01 (dd, J=8.1, 1.6 Hz, 1H); 8.6 (dd, J=4.5, 1.6 Hz, 1H); 7.39-7.32 (m, 5H); 7.32-7.27 (m, 1H); 4.96 (t, J=7.3 Hz, 3H); 3.07 (s, 3H); 3.05-2.91 (m, 2H); 1.88 (s, 3H). m/z=518.1 (M+H).

Provenance & Evidence