Cobalt-Catalyzed Electrophilic Amination of Aryl- and Heteroarylzinc Pivalates with N-Hydroxylamine Benzoates

Chen, Yi-Hung; Grassl, Simon und Knochel, Paul (2018): Cobalt-Catalyzed Electrophilic Amination of Aryl- and Heteroarylzinc Pivalates with N-Hydroxylamine Benzoates. In: Angewandte Chemie-International Edition, Bd. 57, Nr. 4: S. 1108-1111

Abstract

Aryl- and heteroarylzinc pivalates can be aminated with O-benzoylhydroxylamines at 25 degrees C within 2-4 h in the presence of 2.5-5.0% CoCl2 center dot 2LiCl to furnish the corresponding tertiary arylated or heteroarylated amines in good yields. This electrophilic amination also provides access to diarylamines and aryl(heteroaryl)amines. A new tuberculosis drug candidate (Q203) was prepared in six steps and 56% overall yield by using this cobalt-catalyzed amination as the key step.

• Dokumententyp: Zeitschriftenartikel
• Fakultät: Chemie und Pharmazie > Department Chemie
• Themengebiete: 500 Naturwissenschaften und Mathematik > 540 Chemie
• ISSN: 1433-7851
• Sprache: Englisch