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



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.


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Experimentals and data for publication