反应详情

A mixture of methyl 5-(6-bromo-1-oxo-1H-isochromen-3-yl)pentanoate (1.5 g, 4.42 mmol) in 7 N ammonia in MeOH (63.2 ml, 442 mmol, 100.0 equiv.) was left standing at room temperature overnight. The mixture was concentrated, diluted with EtOAc, and added 1 N HCl until pH 4. The mixture was vigorously stirred for 10 min, extracted with EtOAc (2×20 mL), washed with brine, dried over Na2SO4, filtered and evaporated to dryness to yield 1.26 g of methyl 5-(6-bromo-1-oxo-1,2-dihydroisoquinolin-3-yl)pentanoate which was used as such without any further purification.

1. waitwas left
2. concentrationThe mixture was concentrated
3. additiondiluted with EtOAc
4. additionadded 1 N HCl until pH 4
5. extractionextracted with EtOAc (2×20 mL)
6. washwashed with brine
7. dry with materialdried over Na2SO4
8. filtrationfiltered
9. customevaporated to dryness