Hydrochloric Acid → HCID 86727612, compound

Participants

Reaction Steps

A solution of (2S,5R)-4-[(R)-7-(2-fluoro-phenyl)-4-methyl-3-oxo-2,3,4,10-tetrahydro-9-oxa-1,2,4a-triaza-phenanthren-6-yl]-2,5-dimethyl-piperazine-1-carboxylic acid tert-butyl ester (isomer 2, SFC (Table 1, Method 55), Rt=5.643 min., 0.05 g, 0.095 mmol) in HCl (4 M in EtOAc, 2 mL) was stirred at ambient temperature for 1 h. The solvent was concentrated in vacuo to give (R)-6-((2R,5S)-2,5-dimethyl-piperazin-1-yl)-7-(2-fluoro-phenyl)-4-methyl-2,10-dihydro-9-oxa-1,2,4a-triaza-phenanthren-3-one hydrochloride (0.040 g, 99%) as a white solid. 1H NMR (CD3OD, 400 MHz) δ 7.27-7.40 (m, 1H), 7.22-7.26 (m, 2H), 7.15-7.22 (m, 1H), 7.05 (s, 1H), 6.96 (s, 1H), 4.90-4.91 (m, 1H), 4.59-4.70 (m, 2H), 3.09-3.25 (m, 3H), 3.03 (m, 1H), 2.78-2.87 (m, 1H), 2.49 (m, 1H), 1.49 (d, J=6.5 Hz, 3H), 1.24 (d, J=6.5 Hz, 3H), 0.76 (d, J=6.3 Hz, 3H). LC/MS (Table 1, Method 4) Rt=1.739 min.; MS m/z: 424 [M+H]+. SFC (Table 1, Method 55), Rt=6.795 min.

Provenance & Evidence