Combining Incompatible Processes for Deracemization of a Praziquantel Derivative under Flow Conditions

نویسندگان

چکیده

An efficient deracemization method for conversion of the racemate to desirable (R)-enantiomer Praziquantel has been developed by coupling incompatible racemization and crystallization processes. By a library approach, derivative that crystallizes as conglomerate identified. Racemization occurs via reversible hydrogenation over palladium on carbon (Pd/C) packed column at 130 °C, whereas is achieved alternating crystal growth/dissolution steps with temperature cycling between 5–15 °C. These processes are combined means flow system resulting in complete solid phase desired (98 % ee). Such an unprecedented decoupled crystallization/racemization approach can readily be turned into practical process opens new opportunities development essential enantiomerically pure building blocks require harsh methods racemization.

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ژورنال

عنوان ژورنال: Angewandte Chemie

سال: 2021

ISSN: ['1521-3773', '1433-7851', '0570-0833']

DOI: https://doi.org/10.1002/anie.202013502