Trifluoroacetic acid → HCID 86762164, compound

Participants

Reaction Steps

A solution of tert-butyl ((4aR,7aR)-7a-(5-(5-(difluoromethoxy)picolinamido)-2-fluorophenyl)-4a,5,6,7a-tetrahydro-4H-furo[2,3-d][1,3]thiazin-2-yl)carbamate (6 mg, 0.011 mmol) and TFA (17.17 μL, 0.223 mmol) in DCM (111 μL) was stirred at rt for 3 h, and the solvents were removed to give N-(3-((4aR,7aR)-2-amino-4a,5,6,7a-tetrahydro-4H-furo[2,3-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-(difluoromethoxy)picolinamide (7 mg) as its TFA salt as a colorless oil. 1H NMR (500 MHz, METHANOL-d4) 8.60 (br. s., 1H), 8.29 (br. s., 1H), 8.18 (dd, J=7.1, 2.7 Hz, 1H), 7.94-7.87 (m, 1H), 7.84 (dd, J=8.6, 1.6 Hz, 1H), 7.31-7.22 (m, 1H), 7.10 (t, J=75 Hz, 1H), 4.33-4.19 (m, 2H), 3.46 (dd, J=13.6, 3.8 Hz, 1H), 3.34-3.25 (m, 1H), 3.18-3.09 (m, 1H), 2.32 (q, J=7.0 Hz, 2H). MS (M+H)+: 439.11.

Provenance & Evidence