反应详情

温度

20 °C

A mixture of (3S,4S)-4-[(R)-7-(2-fluoro-phenyl)-4-methyl-3-oxo-2,3,4,10-tetrahydro-9-oxa-1,2,4a-triaza-phenanthren-6-yl]-3-methyl-piperidine-1-carboxylic acid tert-butyl ester (0.035 g, 0.069 mmol) in HCl (4 M in EtOAc, 10 mL) was stirred at 20° C. for 2 h. The reaction mixture was concentrated in vacuo to give (R)-7-(2-fluoro-phenyl)-4-methyl-6-((3S,4S)-3-methyl-piperidin-4-yl)-2,10-dihydro-9-oxa-1,2,4a-triaza-phenanthren-3-one hydrochloride acid as a colorless solid (0.015 g, 53%). 1H NMR (400 MHz, MeOD) δ 7.52-7.41 (m, 1H), 7.35-7.18 (m, 3H), 6.93 (s, 1H), 6.86 (s, 1H), 4.90 (m, 1H), 4.65 (s, 2H), 3.47 (m, 1H), 3.22-2.94 (m, 4H), 2.84 (d, J=9.8 Hz, 1H), 2.55-2.27 (m, 2H), 2.00-1.80 (m, 3H), 1.51 (d, J=6.4 Hz, 3H), 1.00-0.80 (m, 3H). SFC (Table 1, Method 43), Rt=3.789 min., LC/MS (Table 1, Method 4) Rt=1.748 min.; MS m/z: 409 [M+H]+.

1. concentrationThe reaction mixture was concentrated in vacuo