Ethanolamine → HCID 68503865, compound

Participants

Reaction Conditions

Reaction Steps

Ethanolamine (3.0 mL, 49.85 mmol) is added to a solution of methanesulfonic acid 2-hydroxy-2-{4-[5-(2-isopropylamino-6-methyl-pyrimidin-4-yl)-[1,2,4]oxadiazol-3-yl]-phenyl}-ethyl ester (152 mg, 0.35 mmol) in dioxane (2.0 mL). The reaction mixture is stirred at 80° C. for 18 h, is then evaporated and purified by prep. TLC (eluting with DCM/MeOH 10:1) to give 99 mg of the title compound as a yellow oil; LC-MS: tR=0.74 min; [M+H]+=399.07. 1H NMR (CDCl3) δ 1.29 (d, J=6.5 Hz, 6H), 2.48 (s, 3H), 2.84 (m, 3H), 2.97 (dd, J=12.3, 3.5 Hz, 1H), 3.73 (t, J=5.0 Hz, 1H), 4.31 (m, 1H), 4.85 (dd, J=8.8, 3.3 Hz, 1H), 5.30 (s br, 1H), 7.29 (s, 1H), 7.53 (d, J=8.3 Hz, 2H), 8.17 (d, J=8.0 Hz, 2H).

Provenance & Evidence