Affiliation:
1. Medicinal Chemistry, Research and Early Development Respiratory and Immunology BioPharmaceuticals R&D, AstraZeneca Gothenburg Sweden
Abstract
AbstractC7‐Arylated pyrazolo[1,5‐a]azines are important structural motifs with profound applications in drug and material research. Here, we report a general and straighforward synthesis of these bi(hetero)aryls via palladium‐catalyzed direct C−H arylation, employing low‐cost and abundant (hetero)aryl chlorides as the aryl source. The catalytic system is robust and covers a wide substrate scope regarding heteroarenes as well as (hetero)aryl chlorides, with possible extension to the C−H arylation of [1,2,4]triazolo[1,5‐a]pyrimidines. This study also presents a rare example of using (hetero)aryl chlorides for the direct C−H arylation of six‐membered heteroarenes.
Subject
General Chemistry,Catalysis,Organic Chemistry