反应详情

3-Chloro-4-[(6,7-dimethoxy-4-quinazolinyl)oxy]aniline (42 mg) was dissolved in chloroform (2.0 ml) and triethylamine (0.13 ml) to prepare a solution. A solution of triphosgene (19 mg) in chloroform was then added to the solution, and the mixture was stirred at room temperature for 5 min. Next, 3-amino-5-methylisoxazole (14 mg) was added thereto, and the mixture was further stirred at room temperature overnight. Water was added to the reaction solution, and the mixture was subjected to separatory extraction with chloroform. The organic layer was concentrated and was evaporated to dryness. Diethyl ether was added to the resultant solid, and the solution was filtered. The filtrate was concentrated, and methyl alcohol was added to the residue. The resultant crystal was collected by filtration to give the title compound (8.8 mg, yield 15%).

1. stirringthe mixture was further stirred at room temperature overnight
2. extractionthe mixture was subjected to separatory extraction with chloroform
3. concentrationThe organic layer was concentrated
4. customwas evaporated to dryness
5. additionDiethyl ether was added to the resultant solid
6. filtrationthe solution was filtered
7. concentrationThe filtrate was concentrated
8. additionmethyl alcohol was added to the residue
9. filtrationThe resultant crystal was collected by filtration