Methylamine → HCID 86679018, compound

Participants

Reaction Steps

The intermediate from Step A above (190 mg, 0.337 mmol), methylamine (2M in THF) (0.843 mL, 1.687 mmol) and THF (2 mL) were sealed in a microwave tube and subjected to microwave irradiation at 150° C. for 3 h. The reaction mixture was partitioned between brine and EtOAc. The combined organic extracts were dried (Na2SO4), filtered and concentrated in vacuo to afford a dark solid. The residue was purified by reverse phase preparative HPLC to give the title product, as a solid. 1H NMR (500 MHz, DMSO-d6): δ 11.35 (s, 1H); 8.87 (d, J=8.1 Hz, 1H); 8.64-8.62 (m, 1H); 7.39 (dd, J=8.1, 4.5 Hz, 1H); 6.61 (d, J=4.9 Hz, 1H); 4.88 (t, J=6.8 Hz, 2H); 4.12-4.07 (m, 2H); 3.04-2.90 (m, 5H); 1.61 (s, 3H); 1.09 (t, J=7.1 Hz, 3H). m/z=514.1 (M+H).

Provenance & Evidence