反应详情

温度

50 °C

2-Fluorophenylisothiocyanate (92 μL, 0.75 mmol) was added to a stirred suspension of 2-hydrazino-N-(4-morpholin-4-ylphenyl)-2-oxoacetamide (Intermediate 16, 160 mg, 0.6 mmol) in DMF (10 mL) and stirred at 50° C. until a clear solution was obtained. PS-Carbodiimide (909 mg, 1.2 mmol) was added and the reaction was heated at 80° C. for a further 4 h. The reaction was filtered and the resin washed with DMF (5 mL). The combined DMF solutions were concentrated in vacuo and the residue triturated with diethyl ether to give the title compound as a yellow powder (190 mg, 82%):

1. customwas obtained
2. temperaturethe reaction was heated at 80° C. for a further 4 h
3. filtrationThe reaction was filtered
4. washthe resin washed with DMF (5 mL)
5. concentrationThe combined DMF solutions were concentrated in vacuo
6. customthe residue triturated with diethyl ether