反应详情

A mixture of 3-(7-bromo-4-methyl-3-oxo-2,3,4,10-tetrahydro-9-oxa-1,2,4a-triaza-phenanthren-6-yloxy)-azetidine-1-carboxylic acid tert-butyl ester (0.080 g, 0.17 mmol), cyclopropyl boronic acid (0.044 g, 0.52 mmol), K2CO3 (0.047 g, 0.34 mmol) and Pd(dppf)Cl2.CH2Cl2 (0.014 g, 0.017 mmol) in dioxane (3 mL) and H2O (0.5 mL) was stirred at 100° C. for 15 h. The mixture was cooled to ambient temperature and the solvent was removed in vacuo. The residue was purified by preparative HPLC (Table 3, Method 4) to give 3-(7-cyclopropyl-4-methyl-3-oxo-2,3,4,10-tetrahydro-9-oxa-1,2,4a-triaza-phenanthren-6-yloxy)-azetidine-1-carboxylic acid tert-butyl ester as a pale yellow solid (0.029 g, 33%). LC/MS (Table 1, Method 2) Rt=1.228 min.; MS m/z: 429 [M+H]+.

1. customthe solvent was removed in vacuo
2. customThe residue was purified by preparative HPLC (Table 3, Method 4)