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Intramolecular Palladium(II)/(IV) Catalysed C(sp3)–H Arylation of Tertiary Aldehydes using a Transient Directing Group

DOI: 10.14469/hpc/5614 Metadata

Created: 2019-05-10 13:31

Last modified: 2019-12-18 09:14

Author: Sahra St John-Campbell

License: Creative Commons: Public Domain Dedication 1.0

Funding: (none given)

Co-author: James A. Bull

Description

Palladium catalysed β-C(sp3)–H activation of tertiary aldehydes using a transient imine directing group enables intramolecular arylation to form substituted indane-aldehydes. A simple amine bearing a methyl ether (2-methoxyethan-1-amine) was the optimal TDG to promote C–H activation and reaction with a proximal C–Br bond. Various substituted derivatives are prepared and the aldehyde functionality is exploited to derivatise the products. Preliminary mechanistic studies identify a reversible C–H activation, product inhibition and suggest that oxidative addition is the turnover limiting step.

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DOIDescription
10.14469/hpc/5618 4. Mechanistic experiments
10.14469/hpc/5616 2. Products 4 and 18-25
10.14469/hpc/5615 1. Substrates 1-3 and 5-16
10.14469/hpc/5617 3. Derivatives 27-30

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