Dehydrogenative Syntheses of Biazoles via a “Pre-Join” Approach

The structural motif
of biazoles is the predominant substructure
of many natural products, pharmaceuticals, and organic materials.
Considerable efforts have focused on synthesizing these compounds;
however, a limited number of processes have been reported for the
efficient formation of biazoles. Herein, we report a “pre-join”
approach for the dehydrogenative synthesis of biazoles, which are
challenging to prepare using conventional methods. A bench-stable
and easily synthesized pyrazine-based group is critical for this transformation.
This strategy enables the homocoupling of biazoles and the heterocoupling
of two different azoles. Due to the broad substrate scope, this strategy
exhibits potential for use in other fields, such as medicine, materials,
and natural product chemistry.