反应详情

温度

110 °C

4-(4-chloro-5-trifluoromethyl-pyrimidin-2-ylamino)-3-methoxy-benzoic acid (5 g) is suspended in toluene (150 mL) and combined with thionyl chloride (1.77 mL), stirred for 2 h at 110° C. and after cooling the solvent is eliminated in vacuo. The residue is taken up in THF (50 mL), cooled to 0° C. and a solution of 4-amino-1-methylpiperidine (1.396 g) and diisopropylethylamine (4.19 mL) is added dropwise thereto. Then the reaction mixture is left to warm up to RT and stirred overnight. After filtering, the residue is dried overnight at 50° C.

1. temperatureafter cooling the solvent
2. temperaturecooled to 0° C.
3. waitThen the reaction mixture is left
4. temperatureto warm up to RT
5. stirringstirred overnight
6. filtrationAfter filtering
7. customthe residue is dried overnight at 50° C.