Metal-Free Synthesis of Functionalized Quinolines from 2-Styrylanilines and 2-Methylbenzothiazoles/2-Methylquinolines

A facile functionalization of C(sp3)-H bonds and tandem cyclization strategy to synthesize quinoline derivatives from 2-methylbenzothiazoles or 2-methylquinolines and 2styrylanilines has been developed. This work avoids the requirement for transition metals, offering a mild approach to activation of C(sp(3))-H bonds and formation of new C-C and C-N bonds. This strategy features excellent functional group tolerance and scaled-up synthetic capability, thus providing an efficient and environmentally friendly access to medicinally valuable quinolines.

Automated summary

A facile method for the functionalization of C(sp3)-H bonds and tandem cyclization to synthesize quinoline derivatives has been developed. This strategy offers a mild approach without the need for transition metals, enabling the activation of C(sp(3))-H bonds and the formation of new C-C and C-N bonds. It has excellent functional group tolerance and scaled-up synthetic capability, providing an efficient and environmentally friendly access to medicinally valuable quinolines.