Direct Approach to 3-Fluoroindoles and 3,3-Difluoroindolines from 2,2-Difluoro-2-phenylethan-1-amines via C-H/N-H Coupling

Herein, a direct method for the synthesis of 3-fluoroindoles and 3,3-difluoroindolines from easily accessible 2,2-difluoro-2-phenylethan1-amines is presented. This protocol was performed by Pd-catalyzed direct C-H/N-H coupling and employed picolinamide as a directing group. By controlling the temperature for this transformation, various 3,3-difluoroindolines and 3-fluoroindoles could be isolated with moderate to good yields.

Automated summary

A direct method for synthesizing 3-fluoroindoles and 3,3-difluoroindolines from easily accessible compounds has been presented in this study. By controlling the reaction temperature, various 3,3-difluoroindolines and 3-fluoroindoles could be isolated with moderate to good yields.