反应详情

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).

1. stirringstirred for 30 minutes at 100° C. in microwave
2. filtrationThe resulting precipitate was filtered
3. washwashed with EtOAc
4. customdried under vacuum