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Application of Daugulis copper-catalyzed direct arylation to the synthesis of 5-aryl benzotriazepines.

ABSTRACT: A method for the direct arylation of benzotriazepines is reported, employing an aryl iodide as the coupling partner, copper iodide as the catalyst, and lithium tert-butoxide as the base. A variety of electron-rich, electron-poor, and sterically hindered aryl iodides are compatible with the reaction conditions. The arylation reaction can also be performed outside a glovebox in air without a significant decrease in yield. Furthermore, convenient microwave conditions for carrying out this transformation are reported.

SUBMITTER: Yotphan S

PROVIDER: S-EPMC2674648 | biostudies-literature | 2009 Apr

REPOSITORIES: biostudies-literature

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Application of Daugulis copper-catalyzed direct arylation to the synthesis of 5-aryl benzotriazepines.

Yotphan Sirilata S Bergman Robert G RG Ellman Jonathan A JA

Organic letters 20090401 7

A method for the direct arylation of benzotriazepines is reported, employing an aryl iodide as the coupling partner, copper iodide as the catalyst, and lithium tert-butoxide as the base. A variety of electron-rich, electron-poor, and sterically hindered aryl iodides are compatible with the reaction conditions. The arylation reaction can also be performed outside a glovebox in air without a significant decrease in yield. Furthermore, convenient microwave conditions for carrying out this transform ...[more]

PMID: 19260648

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