The Ireland–Claisen rearrangement strategy towards the synthesis of the schizophrenia drug, (+)-asenapine?

Organic & Biomolecular Chemistry Pub Date: 2015-11-27 DOI: 10.1039/C5OB02047F

Abstract

(±)-Asenapine, sold in the market as Saphris/Sycrest for the treatment of bipolar disorders, is synthesized in an optically pure form involving an Ireland–Claisen rearrangement as the key step. This approach allows access to all diastereomers.

Graphical abstract: The Ireland–Claisen rearrangement strategy towards the synthesis of the schizophrenia drug, (+)-asenapine
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