Access to Hetero-Benzyl Scaffolds via Transient-Ligand-Enabled Direct γ-C(sp3)-H Arylation of 3-Methylheteroarene-2-Carbaldehydes.

doi:10.1021/acs.joc.0c00154

Paper

Access to Hetero-Benzyl Scaffolds via Transient-Ligand-Enabled Direct γ-C(sp3)-H Arylation of 3-Methylheteroarene-2-Carbaldehydes.

Published Apr 29, 2020 · C. Reddy, Javed Y. Shaikh, Ramakrishna G. Bhat

The Journal of organic chemistry

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8

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0

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Abstract

An efficient and straightforward method has been developed for the synthesis of β-benzyl-substituted five-membered heterocyclic carbaldehydes via transient directing group-enabled direct γ-C(sp3)-H arylation of 3-methylheteroarene-2-carbaldehydes. A wide range of 3-methylheteroarene carbaldehydes undergoes coupling with a variety of aryl iodides including less reactive iodo pyridine derivatives to provide a library of highly selective functionalized products in good to excellent yields. Some of these products have been successfully utilized in synthesizing useful synthetic intermediates.

Study Snapshot

This study developed an efficient method for synthesis of -benzyl-substituted five-membered heterocyclic carbaldehydes, providing a library of highly selective functionalized products in good to excellent yields for synthetic intermediates.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Access to Hetero-Benzyl Scaffolds via Transient-Ligand-Enabled Direct γ-C(sp3)-H Arylation of 3-Methylheteroarene-2-Carbaldehydes.

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