Iridium(I)-Catalyzed α-C(sp³)-H Alkylation of Saturated Azacycles.

ABSTRACT: Saturated azacycles are commonly encountered in bioactive compounds and approved therapeutic agents. The development of methods for functionalization of the α-methylene C-H bonds of these highly privileged building blocks is of great importance, especially in drug discovery. While much effort has been dedicated toward this goal by using a directed C-H activation approach, the development of directing groups that are both general as well as practical remains a significant challenge. Herein, the design and development of novel amidoxime directing groups is described for Ir(I)-catalyzed α-C(sp³)-H alkylation of saturated azacycles using readily available olefins as coupling partners. This protocol extends the scope of saturated azacycles to piperidines, azepane, and t

SUBMITTER: Verma P 

PROVIDER: S-EPMC7219544 | biostudies-literature | 2020 Mar

REPOSITORIES: biostudies-literature