Copper‐Catalyzed N1 Coupling of 3‐Aminoindazoles and Related Aminoazoles with Aryl Bromides. Issue 4 (30th November 2021)

• Record Type: Journal Article
• Authors: Cyr, Patrick; Joseph‐Valcin, Eve‐Marline; Boissarie, Patrick; Simoneau, Bruno; Marinier, Anne
• Is Part Of: European journal of organic chemistry. Volume 2022:Issue 4(2022)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2021-11-30
• Subjects: Aminoindazoles -- Arylation -- Copper catalysis -- Homogeneous catalysis -- Regioselectivity; Chemistry, Organic -- Periodicals; Organic compounds -- Synthesis -- Periodicals; Bioorganic chemistry -- Periodicals; Chemistry, Physical organic -- Periodicals; 547
• DOI: 10.1002/ejoc.202101245
• Languages: English
• ISSNs: 1434-193X

Abstract

Abstract: The N 1 ‐selective arylation of 3‐aminoindazoles using copper catalysis is herein reported. The reaction uses readily accessible aryl bromides as coupling partners, including those from heterocycles, and allows easy access to a broad variety of substituted 3‐aminoindazoles. The methodology was also examined on other aminoazoles of interest for the pharmaceutical industry. Abstract : A coupling between 3‐aminoindazoles and aryl bromides, selectively occurring at the N 1 position, was developed using copper catalysis. The transformation allows the use of a variety of heterocycles for both coupling partners and provides rapid access to arylated aminoazoles of high interest in drug discovery.