Solution to the C-3-Arylation of Indazoles: Development of a Scalable Method

• Published in: Organic letters Vol. 18; no. 13; pp. 3218 - 3221
• Main Authors: Basu, Kallol, Poirier, Marc, Ruck, Rebecca T.
• Format: Journal Article
• Language: English
• Published: WASHINGTON Amer Chemical Soc 01.07.2016
• Subjects: Chemistry; Chemistry, Organic; Physical Sciences; Science & Technology; ACIDS; ARYLATION; EFFICIENT SYNTHESIS; PROTOCOL; C-3; 1H-INDAZOLES; ARYL; INHIBITORS

3-(Hetero)arylindazoles are important motifs in several biologically active compounds. Mild and flexible palladium-mediated Negishi reaction conditions are reported for the introduction of (hetero)aryl moieties at the 3-position of N(2)-SEM-protected indazoles in high yields. The requisite Lion and...