An approach to chemoenzymatic DKR of amines in Soxhlet apparatus

• Coexistence of thermolabile enzyme and heat-activated racemization catalyst for DKR of amines is enabled by Soxhlet-extractor reactor setup.
• Proof-of-concept study demonstrates feasibility of the approach.
• (R)-1-(Phenyl)ethylamine is obtained from the racemic precursor in 65–70% yield and 99% ee.
• At present stage, the generality of the approach is limited by side-product formation by sec-amine dimerization.

The coexistence of thermolabile enzyme and metal catalyst for racemization of amines in chemoenzymatic dynamic kinetic resolution, requiring high temperature of operation, is enabled by carrying out the reaction in modified Soxhlet extraction system. Initial insights into the scope and limitations of the developed reaction system are discussed.

The coexistence of thermolabile enzyme and metal catalyst for racemization of amines in chemoenzymatic dynamic kinetic resolution, requiring high temperature of operation, is enabled by carrying out the reaction in modified Soxhlet extraction system.Figure optionsDownload as PowerPoint slide