C1 − H morpholinomethylation and formylation of pyrrolo[1,2-<i>a</i>]quinoxalines

We report two methods for selective morpholinomethylation and formylation of C1 − H bonds in pyrrolo[1,2-<i>a</i>]quinoxalines. Reaction of pyrrolo[1,2-<i>a</i>]quinoxalines and morpholine using CuI catalyst, (bis(trifluoroacetoxy)iodo)benzene oxidant, and DMSO solvent yielded the morpholinomethylation products. Meanwhile, formylation of C1 − H bonds in pyrrolo[1,2-<i>a</i>]quinoxalines progressed in the presence of CuI catalyst, trifluoroacetic acid, and DMSO solvent. Compounds bearing halogen, methylsulfonyl, pyridine, and thiophene groups were isolated in moderate yields.