Hydrochloric Acid → HCID 49821589, compound

Participants

Reaction Steps

Diethyl [4-({4-[({2-[methyl(methylsulfonyl)amino]pyridin-3-yl}methyl)amino]-5-(trifluoromethyl)pyrimidin-2-yl}amino)phenyl]phosphonate (Example 2) in an excess of concentrated HCl (37%) and heated at 80° C. for 5 h. The reaction mixture was concentrated in vacuo and the residue purified by preparative HPLC (MDP) to afford the title compound (Example 40). 1H NMR (400 MHz, DMSO-d6) δ ppm 1.15 (t, J=6.9 Hz, 3H), 3.16 (s, 6H), 3.81 (ddd, J=14.7, 7.3, 7.1 Hz, 2H), 4.83 (d, J=5.6 Hz, 2H), 7.34-7.45 (m, 3H), 7.55 (dd, J=8.2, 3.2 Hz, 2H), 7.64-7.73 (m, 2H), 8.31 (d, J=0.8 Hz, 1H), 8.45 (dd, J=4.7, 1.9 Hz, 1H), 9.86 (s, 1H); MS (UPLC TOF): m/z 562.14 [MH+]; HPLC: tR=1.15 min (polar-3).

Provenance & Evidence