HCID 86727506, compound → HCID 86727507, compound

Participants

Reaction Steps

A solution of 3-{(R)-1-[(R)-7-(2-fluoro-phenyl)-4-methyl-3-oxo-2,3,4,10-tetrahydro-9-oxa-1,2,4a-triaza-phenanthren-6-yl]-ethyl}-3-methyl-azetidine-1-carboxylic acid tert-butyl ester (0.073 g, 0.144 mmol) in HCl (4M in EtOAc, 1 mL) was stirred at ambient temperature for 1 h. The reaction mixture was concentrated in vacuo to give (R)-7-(2-fluoro-phenyl)-4-methyl-6-[(R)-1-(3-methyl-azetidin-3-yl)-ethyl]-2,10-dihydro-9-oxa-1,2,4a-triaza-phenanthren-3-one (0.06 g, 100%), which was used directly in the next step without further purification. 1H NMR (CD3OD, 400 MHz): δ 7.45 (m, 1H), 7.16-7.34 (m, 3H), 6.90-6.96 (m, 1H), 6.86 (s, 1H), 4.92-4.98 (m, 1H), 4.57-4.68 (m, 2H), 4.24 (m, 1H), 3.69-3.76 (m, 1H), 3.46-3.55 (m, 1H), 3.38 (m, 1H), 2.97 (m, 1H), 1.36-1.51 (m, 6H), 1.20-1.27 (m, 3H). LC/MS (Table 1, Method 25) Rt=0.673 min; MS (ESI): m/z 409 [M+H]+.

Provenance & Evidence