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Pd-Catalyzed highly selective and direct ortho C−H arylation of pyrrolo[2,3-d]pyrimidine derivatives

Abstract

The first Pd-catalyzed one-pot direct ortho C−H arylation of pyrrolo[2,3-d]pyrimidine derivatives is reported. Many functional groups are well tolerated under this direct C−H arylation condition. This protocol provides a variety of biphenyl-containing pyrrolo[2,3-d]pyrimidines in good to excellent yields, which are potentially of great importance in medicinal chemistry. Diarylation and heteroarylation were both demonstrated to be effective and this methodology was also proved practical by the gram-scale synthesis.

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Publication details

The article was received on 28 Oct 2019, accepted on 29 Nov 2019 and first published on 02 Dec 2019


Article type: Research Article
DOI: 10.1039/C9QO01312A
Org. Chem. Front., 2019, Accepted Manuscript

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    Pd-Catalyzed highly selective and direct ortho C−H arylation of pyrrolo[2,3-d]pyrimidine derivatives

    J. Zhou, Z. Mao, H. Pan and X. Zhang, Org. Chem. Front., 2019, Accepted Manuscript , DOI: 10.1039/C9QO01312A

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