反应详情

The mixture of 5.39 g of 4-amino-2-chloro-6,7,8-trimethoxy-quinazoline, 4.32 g of 2-(4-piperidinyl)-isoindolin-1-one, 4.24 g of anhydrous sodium carbonate and 75 ml of dimethylformamide is stirred under nitrogen at 125°-130° for 16 hours. It is filtered, the filtrate evaporated, the residue dissolved in methylene chloride and the solution washed with aqueous sodium bicarbonate. The organic layer is separated, dried, and evaporated. The residue is suspended in refluxing isopropanol and acidified with hydrogen chloride to pH=1. The precipitate formed is filtered off and triturated with warm ethanol to yield the 2-[1-(4-amino-6,7,8-trimethoxy-2-quinazolinyl)-4-piperidinyl]-isoindolin-1-one monohydrochloride melting at 234° (dec.).

1. filtrationIt is filtered
2. customthe filtrate evaporated
3. dissolutionthe residue dissolved in methylene chloride
4. washthe solution washed with aqueous sodium bicarbonate
5. customThe organic layer is separated
6. customdried
7. customevaporated
8. temperaturein refluxing isopropanol
9. customThe precipitate formed
10. filtrationis filtered off
11. customtriturated with warm ethanol