An Innovative Approach for the Synthesis of 7-Hydroxyquinolin-2(1H)-one: A Key Intermediate of Brexpiprazole

摘要

2,3-Dichloro-5,6-dicyano-p-benzoquinone (DDQ) mediated oxidation of 7-hydroxy-l,2,3,4-tetrahydro-2-quinolinone has been prepared I from 3-hydroxy aniline to obtain 7-hydroxyquinolin-2(1H)-one in aqueous media. Stoichiometric quantities of DDQ and THF provides a high out put of 7-hydroxyquinolin-2(1H)-one and reduces the consumption of organic solvents and discourages by-products. Overall advantage with this approach was reduce the time cycle and cost of the brexpiprazole intermediate.