反应详情

温度

0 °C

N1-{4-[(6,7-Dimethoxy-4-quinazolinyl)oxy]phenyl}-2-phenoxyacetamide (200 mg) was dissolved in tetrahydrofuran (10 ml) to prepare a solution. A 1 M solution (1.3 ml) of a borane-tetrahydrofuran complex in tetrahydrofuran was then added to the solution, and the mixture was stirred with heating under reflux for 2 hr. The reaction solution was cooled to 0° C. and was adjusted to pH=1 by the addition of 1 N hydrochloric acid, followed by stirring with heating under reflux for 30 min. The reaction solution was cooled to 0° C., was adjusted to pH=12 by the addition of a 1 N aqueous sodium hydroxide solution, and was extracted with chloroform. After the concentration of the extract, the residue was purified on a column using chloroform/methanol to give the title compound (155 mg, yield 80%).

1. customto prepare a solution
2. temperaturewith heating
3. temperatureunder reflux for 2 hr
4. stirringby stirring
5. temperaturewith heating
6. temperatureunder reflux for 30 min
7. temperatureThe reaction solution was cooled to 0° C.
8. extractionwas extracted with chloroform
9. customAfter the concentration of the extract, the residue was purified on a column