Trifluoroacetic acid → (R)-1-methyl-9-((3-methylazetidin-3-yl)amino)-8-(trifluoromethyl)-3,5-dihydrobenzo[5,6][1,4]oxazino[3,4-c][1,2,4]triazin-2(1H)-one trifluoroacetic acid

Participants

Reaction Steps

To a solution of (R)-tert-butyl 3-methyl-3-((1-methyl-2-oxo-8-(trifluoromethyl)-1,2,3,5-tetrahydrobenzo[5,6][1,4]oxazino[3,4-c][1,2,4]triazin-9-yl)amino)azetidine-1-carboxylate (Enantiomer 1, SFC (Table 1, Method 16) Rt: 6.686 min, 0.270 g, 0.55 mmol) in DCM (10 mL) was added TFA (2 mL) and the mixture was stirred at ambient temperature for 2 h. The solvent was removed in vacuo to give (R)-1-methyl-9-((3-methylazetidin-3-yl)amino)-8-(trifluoromethyl)-3,5-dihydrobenzo[5,6][1,4]oxazino[3,4-c][1,2,4]triazin-2(1H)-one trifluoroacetic acid (Example #100-1, Enantiomer 1, SFC (Table 1, Method 18) Rt: 9.62 min, 0.275 g, 99%) as a pale solid. LC/MS (Table 1, Method 5) Rt=2.005 min; MS m/z: 370 [M+H]+.

Provenance & Evidence