反应详情

A solution of 3-((R)-8-ethyl-1-methyl-2-oxo-1,2,3,5-tetrahydro-6-oxa-3,4,10,11b-tetraaza-cyclopenta[b]phenanthren-10-yl)-3-methyl-azetidine-1-carboxylic acid tert-butyl ester (0.04 g, 0.088 mmol) in HCl (4M in EtOAc, 3 mL) was stirred at −5-0° C. for 2 h. The solvent was removed in vacuo to give (R)-8-ethyl-1-methyl-10-(3-methyl-azetidin-3-yl)-3,5-dihydro-10H-6-oxa-3,4,10,11b-tetraaza-cyclopenta[b]phenanthren-2-one hydrochloride (0.0122 g, 39%) as a yellow solid. 1H NMR (400 MHz, methanol-d4): δ 7.22 (s, 1H), 7.06 (s, 1H), 6.78 (s, 1H), 4.95 (m, 1H), 4.75 (m, 2H), 4.63-4.50 (m, 4H), 2.72 (q, J=7.6 Hz, 2H), 1.85 (s, 3H), 1.46 (d, J=6.8 Hz, 3H), 1.33 (t, J=7.6 Hz, 3H). LC/MS (Table 1, Method 4) Rt=1.591 min.; MS m/z: 354 [M+H]+.

1. customThe solvent was removed in vacuo