反应详情

To a solution of 7-({2-[(cyclopropylcarbonyl)amino]pyridin-4-yl}oxy)-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid (3.03 g, 8.61 mmol) in DMF (75 mL), was added DIPEA (4.50 mL, 25.8 mmol) and HATU (4.91 g, 12.9 mmol). The reaction mixture was allowed to stir at rt for 30 min, and then tert-butyl [3-amino-5-(trifluoromethyl)benzyl]carbamate (2.50 g, 8.61 mmol) was added. The reaction mixture was allowed to stir for 18 h. Water was added and the precipitate was filtered, washed with water and hexane and dried under vacuum. The residue was purified by column chromatography to give tert-butyl [3-({[7-({2-[(cyclopropylcarbonyl)amino]pyridin-4-yl}oxy)-1,2,3,4-tetrahydronaphthalen-2-yl]carbonyl}-amino)-5-(trifluoromethyl)benzyl]carbamate (3.80 g, 70.6%) as a yellow solid. LCMS: (FA) ES+ 625.6, ES− 623.4.

1. stirringto stir for 18 h
2. filtrationthe precipitate was filtered
3. washwashed with water and hexane
4. customdried under vacuum
5. customThe residue was purified by column chromatography