Open AccessSynthesis of 2-BMIDA Indoles via Heteroannulation: Applications in Drug Scaffold and Natural Product Synthesis
Author(s) -
George E. Bell,
James W. B. Fyfe,
Eva M. Israel,
Alexandra M. Z. Slawin,
Matthew Campbell,
Allan J. B. Watson
Publication year - 2022
Publication title -
organic letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.94
H-Index - 239
eISSN - 1523-7060
pISSN - 1523-7052
DOI - 10.1021/acs.orglett.2c00959
Subject(s) - chemistry , regioselectivity , indole test , natural product , combinatorial chemistry , aspidosperma , scaffold , drug discovery , stereochemistry , organic chemistry , catalysis , biochemistry , computer science , database
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.
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