01162nas a2200157 4500008004100000022001400041245010200055210006900157260000800226490000700234520056300241100002200804700002500826700002200851856013100873 2023 eng d a1861-472800aBF3.Et2O-catalyzed selective C-4 alkylation of isoquinolin1(2H)-ones employing p-quinone methides0 aBF3Et2Ocatalyzed selective C4 alkylation of isoquinolin12Hones e cSep0 v183 a

The direct C-4 alkylation of isoquinolin-1(2H)-one moiety is a challenging transformation in organic synthesis. Here we present a practical and efficient synthesis of C-4 alkylated isoquinolin-1(2H)-ones through conjugate addition of isoquinolin-1(2H)-ones to p-quinone methides for the first time. The process is facilitated by Lewis acid catalysis and this operationally straightforward, mild, metal-free and one-pot transformation provides a wide range of C-4 alkylated isoquinolin-1(2H)ones at ambient temperature in good to excellent yields.

1 aMore, Devidas, A.1 aGhotekar, Ganesh, S.1 aMuthukrishnan, M. uhttps://library.ncl.res.in/content/bf3et2o-catalyzed-selective-c-4-alkylation-isoquinolin12h-ones-employing-p-quinone-methides