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Updated: Aug 23, 2025

Preparation of Contiguous Bisaziridines for Regioselective Ring-Opening Reactions
Published on: July 28, 2022
Enantioselective synthesis of (-)-tetrabenazine via continuous crystallization-induced diastereomer transformation
Andrew J Kukor1, Noah Depner1, Isabelle Cai1
1Department of Chemistry, The University of British Columbia Vancouver BC V6T 1Z1 Canada.
Abstract:
A multi-well continuous CIDT approach with inline racemization of the solution phase is presented. Using two in-house built PATs and a flow reactor, we were able to successfully crystallize an enantiopure salt of TBZ, the active metabolite of the tardive dyskinesia drug valbenazine. Despite discovering an undesired racemic solid phase, inline racemization combined with careful control of crystallization conditions allowed for multigram quantities of enantiopure material to be harvested using our setup. Critically, this control was made possible by the use of PATs to observe and quantify the composition of both the solid and solution phases.
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