Chemical Engineering and Industrial Chemistry

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

Authors

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.

Version notes

Changed author name from "Cheng-yi-Chen" to Cheng-yi Chen".

Content

Thumbnail image of 2022_06_16 Manuscript Draft.pdf

Supplementary material

Thumbnail image of 2022_06_14 SI.pdf
Supporting information
Experimentals and data for publication