Developing an atroposelective dynamic kinetic resolution of MRTX1719 by resolving incompatible chemical operations

CHEMICAL COMMUNICATIONS(2022)

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摘要
A high-yielding protocol for atropisomeric resolution was developed by rectifying 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 the consumption of solvent and advanced synthetic intermediates.
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关键词
atroposelective dynamic kinetic resolution,mrtx1719,incompatible chemical operations
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