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Simultaneous Processing of Antagonistic Chemical Events (SPACE): An Atroposelective Dynamic Kinetic Resolution of MRTX1719

17 June 2022, Version 1
Working Paper
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

A high-yielding protocol for atropisomeric resolution was developed by rectifying inherent incompatibilities between crystallization and epimerization via continuous processing. Application toward synthesis of MRTX1719, a densely functionalized active pharmaceutical ingredient (API), improved yield from 37% to 87%. This protocol provides a complementary means to access rotamers which challenge current asymmetric methodologies, and greatly improves sustainability by decreasing consumption of solvent and advanced synthetic intermediates.

Keywords

atropisomer
continuous flow
epimerization
crystallization
active pharmaceutical ingredient
DKR

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Version History

Jun 17, 2022 Version 1

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The content is available under CC BY 4.0 [opens in a new tab]

DOI

10.26434/chemrxiv-2022-pwtdx
D O I: 10.26434/chemrxiv-2022-pwtdx [opens in a new tab]

Author’s competing interest statement

The author(s) have declared they have no conflict of interest with regard to this content

Ethics

The author(s) declare that they have sought and gained approval from the relevant ethics committee/IRB for this research and its publication.

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