反应详情

To a solution of 7-[(7-oxo-7,8-dihydro-1,8-naphthyridin-4-yl)oxy]-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid (0.18 g, 0.00053 mol) in DMF (5.3 mL) was added diisopropylethylamine (0.11 mL, 0.00063 mol) and HATU (0.24 g, 0.00063 mol). The reaction mixture was allowed to stir at rt for 1 hr. tert-Butyl [3-amino-5-(trifluoromethyl)benzyl]-carbamate (0.15 g, 0.00053 mol) was added and the reaction mixture was allowed to stir for an additional 15 hr. Water was added to the reaction mixture and a solid precipitated. This solid was collected by filtration and purified by column chromatography to give tert-butyl [3-[({7-[(7-oxo-7,8-dihydro-1,8-naphthyridin-4-yl)oxy]-1,2,3,4-tetrahydronaphthalen-2-yl}carbonyl)amino]-5-(trifluoromethyl)benzyl]carbamate as a white solid (0.24 g, 75%). LCMS: (FA) ES+ 609.4.

1. stirringto stir for an additional 15 hr
2. customa solid precipitated
3. filtrationThis solid was collected by filtration
4. custompurified by column chromatography