1-(3-Aminophenyl)pyrrolidin-2-one → HCID 66712127, compound

Participants

Reaction Steps

Following the synthetic and purification procedures described in Example 1293d, 3-[2-(2-methanesulfinyl-pyrrolo[2,1-f][1,2,4]triazin-7-yl)-pyrrol-1-yl]-propionitrile (93 mg, 0.31 mmol) was coupled to 1-(3-amino-phenyl)-pyrrolidin-2-one (77 mg, 0.44 mmol) at 120° C. for 96 h to afford the title compound. Yield of TFA salt: 23 mg (15%) of brown powder. LC/MS: 412 (M+H); HPLC: 97% pure, RT=2.16 min; mp: 60-67° C.; 1H NMR: (DMSO, δ) 9.55 (s, 1H), 8.99 (s, 1H), 7.89 (s, 1H), 7.51 (d, J=8.2, 1H), 7.28 (d, J=8.2, 1H), 7.20 (t, J=8.1, 1H), 7.14 (m, 1H), 6.95 (d, J=4.5, 1H), 6.88 (d, J=4.4, 1H), 6.49 (dd, J=3.6, 1.5 1H), 6.27 (t, J=3.6, 1H), 4.19 (t, J=6.3, 2H), 3.49 (t, J=7.0, 2H), 2.77 (t, J=6.3, 2H), 2.47 (t, J=7.0, 2H), 2.02 (p, J=7.0, 2H).

Provenance & Evidence