Trifluoroacetic acid → 4-(5-((1,1-Dioxidohexahydro-5H-isothiazolo[2,3-A]pyrazin-5-YL)methyl)-2-((5-fluoro-6-methoxy-3-pyridinyl)amino)-3-pyridinyl)-6-methyl-1,3,5-triazin-2-amine

Participants

Reaction Steps

The title compound was prepared from 4-(5-((1,1-dioxidohexahydro-5H-isothiazolo[2,3-a]pyrazin-5-yl)methyl)-2-((5-fluoro-6-methoxy-3-pyridinyl)amino)-3-pyridinyl)-N,N-bis(4-methoxybenzyl)-6-methyl-1,3,5-triazin-2-amine via the similar deprotection protocol as described previously in Example 178, Step 4, using trifluoroacetic acid and trifluoromethanesulfonic acid and isolated (61 mg, 30%) as a yellow solid. m/z (ESI, +ve ion) 516 (M+H)+. 1H NMR (400 MHz, d6-DMSO) δ 11.95 (s, 1H) 8.73 (d, J=2.15 Hz, 1H) 8.42 (d, J=2.15 Hz, 1H) 8.37 (dd, J=12.81, 2.05 Hz, 1H) 8.26 (d, J=2.15 Hz, 1H) 7.91 (br. s., 1H) 7.76 (br. s., 1H) 3.93 (s, 3H) 3.45-3.62 (m, 1H) 3.00-3.30 (m, 5H) 2.80-3.00 (m, 2H) 2.62-2.74 (m, 1H) 2.44 (s, 3H) 2.23-2.36 (m, 1H) 2.06-2.16 (m, 1H) 1.81-1.96 (m, 2H).

Provenance & Evidence