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Palladium-catalyzed C‒O coupling of amino alcohols for the synthesis of aryl ethers

Larrow, Jay, Mikus, Malte, Sanchez, Carina and Fridrich, Cary (2019) Palladium-catalyzed C‒O coupling of amino alcohols for the synthesis of aryl ethers. Advanced Synthesis & Catalysis, 362 (2). pp. 430-436. ISSN 1615-41501615-4169

Abstract

Amine containing aryl ethers are common pharmacophore motifs that continue to emerge from drug discovery efforts. As amino alcohols are readily available building blocks, practical methodologies for incorporating them into more complex structures are highly desireable. We report our efforts to explore the application of Pd-catalyzed C-O coupling methods to the arylation of 1,2- and 1,3-amino alcohols. We established reliable conditions, under which we explored the scope and limitations of the transformation. The insights gained have been valuable in employing this methodology within a fast-moving drug discovery environment, which we anticipate will be of general interest to the synthesis and catalysis communities.

Item Type: Article
Keywords: amino alcohols; C-O coupling; aryl alkyl ethers; bippyphos; palladium catalyzed
Date Deposited: 28 Feb 2020 00:45
Last Modified: 28 Feb 2020 00:45
URI: https://oak.novartis.com/id/eprint/41115

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