反应详情

A mixture of (5-(3-aminopyridin-2-yloxy)-3,4-dihydroquinolin-1(2H)-yl)(phenyl)methanone (Example A171d) (224 mg, 0.58 mmol), 1,1′-thiocarbonyldi-2(1H)-pyridone (269 mg, 1.16 mmol) in DCM (10 mL) was agitated at rt for 4 h. The mixture was evaporated and diluted in THF (5 mL), pivalamidine (79 mg, 0.58 mmol) and DIPEA (205 μL, 1.16 mmol) were added and mixture was heated at 80° C. in a sealed tube for 24 h. The solution was cooled down and DEAD (183 μL, 1.16 mmol) was added, mixture was stirred for 2 h. The reaction mixture was evaporated in vacuo and purified using preparative HPLC to afford the final product (40 mg). (M+H)+=486.

1. customThe mixture was evaporated
2. additiondiluted in THF (5 mL)
3. temperaturemixture was heated at 80° C. in a sealed tube for 24 h
4. temperatureThe solution was cooled down
5. stirringmixture was stirred for 2 h
6. customThe reaction mixture was evaporated in vacuo
7. custompurified