反应详情

4-{[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]carbamoyl}-3-nitrobenzoic acid (500 mg, 1.11 mmol) in DMF (10 mL) was treated with 1-hydroxybenzotriazole (195 mg, 1.44 mmol), EDCI (276 mg, 1.44 mmol) and 1-methylpiperazine (0.16 mL, 1.44 mmol). The reaction was left at room temperature over night. The volatiles were removed by evaporation, the residue was added drop-wise to iced-water (25 mL) with stirring. A yellow solid was obtained which was extracted with DCM (2×25 mL). The combined organic layers were dried over sodium sulphate and evaporated leaving 590 mg of title compound which was employed in the following step without any further purification.

1. waitThe reaction was left at room temperature over night
2. customThe volatiles were removed by evaporation
3. additionthe residue was added drop-wise to iced-water (25 mL)
4. customA yellow solid was obtained which
5. extractionwas extracted with DCM (2×25 mL)
6. dry with materialThe combined organic layers were dried over sodium sulphate
7. customevaporated