Practical one-pot sequential procedure for the preparation of N-arylated 3,4-disubstituted pyrroles from alkenes

By using tBuONa and Cs2CO3 as a mixed base, van Leusen pyrrole synthesis and copper-catalyzed N-arylation of pyrrole proceeded sequentially in a single flask to give N-arylated 3,4-disubstituted pyrroles smoothly. Thus, a series of desired N-arylated pyrroles were prepared directly from the electron-deficient alkenes.

Graphical abstractBy using tBuONa and Cs2CO3 as a mixed base, van Leusen pyrrole synthesis and copper-catalyzed N-arylation of pyrrole proceeded sequentially in a single flask to give N-arylated 3,4-disubstituted pyrroles smoothly. Thus, a series of desired N-arylated pyrroles were prepared directly from the electron-deficient alkenes.Figure optionsDownload full-size imageDownload as PowerPoint slide