反应详情

A solution of 7-(3-chloropropoxy)-6-methoxy-3-((pivaloyloxy)methyl)-3,4-dihydroquinazolin-4-one (3 g, 7.84 mmol) in 1-methylpiperazine (30 ml) was heated at 100° C. for 1 hour. After cooling, the mixture was partitioned between saturated ammonium chloride and methylene chloride. The organic layer was washed with water, brine, dried (MgSO4) and the volatiles were removed by evaporation. The residue was purified by column chromatography eluting with methylene chloride/methanol (95/5 followed by 90/10). The volatiles were removed by evaporation to give 6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)-3-((pivaloyloxy)methyl)-3,4-dihydroquinazolin-4-one (3.24 g, 92%).

1. temperatureAfter cooling
2. customthe mixture was partitioned between saturated ammonium chloride and methylene chloride
3. washThe organic layer was washed with water, brine
4. dry with materialdried (MgSO4)
5. customthe volatiles were removed by evaporation
6. customThe residue was purified by column chromatography
7. washeluting with methylene chloride/methanol (95/5 followed by 90/10)
8. customThe volatiles were removed by evaporation