Trifluoroacetic acid → 6-(azetidin-3-ylamino)-4(R)-methyl-7-trifluoromethyl-2,10-dihydro-9-oxa-1,2,4a-triaza-phenanthren-3-one trifluoroacetic acid

Participants

Reaction Steps

A solution of 3-(4(R)-methyl-3-oxo-7-trifluoromethyl-2,3,4,10-tetrahydro-9-oxa-1,2,4a-triaza-phenanthren-6-ylamino)-azetidine-1-carboxylic acid tert-butyl ester ((Enantiomer 2, SFC (Table 1, Method 6), Rt=10.53 min., 0.260 g, 0.57 mmol) in DCM (10 mL) and TFA (2 mL) was stirred at ambient temperature for 1 h. The solvent was removed in vacuo to give 6-(azetidin-3-ylamino)-4(R)-methyl-7-trifluoromethyl-2,10-dihydro-9-oxa-1,2,4a-triaza-phenanthren-3-one trifluoroacetic acid as a pale yellow solid (Example #53-2, Enantiomer 2, SFC (Table 1, Method 7), Rt=7.98 min, 0.260 g, 97%). LC/MS (Table 1, Method 5) Rt=2.068 min.; MS m/z: 356 [M+H]+.

Provenance & Evidence