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Synthesis of 2-BMIDA Indoles via Heteroannulation: Applications in Drug Scaffold and Natural Product Synthesis.

ABSTRACT: A Pd-catalyzed heteroannulation approach for the synthesis of C2 borylated indoles is reported. The process allows access to highly functionalized 2-borylated indole scaffolds with complete control of regioselectivity. The utility of the process is demonstrated in the synthesis of borylated sulfa drugs and in the concise synthesis of the Aspidosperma alkaloid Goniomitine.

SUBMITTER: Bell GE

PROVIDER: S-EPMC9062883 | biostudies-literature | 2022 Apr

REPOSITORIES: biostudies-literature

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Synthesis of 2-BMIDA Indoles via Heteroannulation: Applications in Drug Scaffold and Natural Product Synthesis.

Bell George E GE Fyfe James W B JWB Israel Eva M EM Slawin Alexandra M Z AMZ Campbell Matthew M Watson Allan J B AJB

Organic letters 20220415 16

A Pd-catalyzed heteroannulation approach for the synthesis of C2 borylated indoles is reported. The process allows access to highly functionalized 2-borylated indole scaffolds with complete control of regioselectivity. The utility of the process is demonstrated in the synthesis of borylated sulfa drugs and in the concise synthesis of the <i>Aspidosperma</i> alkaloid Goniomitine. ...[more]

PMID: 35426314

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