4-Chlorophenyl Isocyanate → 7-(6-Oxo-5,6-dihydro-benzo[c][1,8]naphthyridin-1-yloxy)-2,3-dihydro-benzo[1,4]oxazine-4-carboxylic acid (4-chloro-phenyl)-amide

Participants

Reaction Steps

Compound 218 (50 mg, 0.14 mmol), 1-chloro-4-isocyanato-benzene (33 mg, 0.22 mmol), and DIEA (0.07 mL, 0.43 mmol) were dissolved in dioxane (2 mL) and stirred and stirred for 30 minutes at 100° C. in microwave. The reaction mixture was diluted with H2O/EtOAc. The resulting precipitate was filtered, washed with EtOAc, and dried under vacuum to provide 220 (51 mg, 71% yield) as a tan solid. LC-MS (M+H=499, obsd.=499).

Provenance & Evidence