U. Stojiljković, Claudio Meyer, Pierre Boulay
Jun 22, 2022
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Journal
Synthesis
Abstract
Morpholine is a heterocyclic moiety widely used in medicinal chemistry as a building block. It has unique physicochemical properties, as it can improve both pharmacokinetic and pharmacodynamic properties of active pharmaceutical ingredients. However, the efficient synthesis of enantiomerically pure morpholine building blocks remains challenging. Herein, we report a synthesis of optically pure 3-hydroxymethylmorpholine building blocks, as well as their sulfamidates, exploiting a stereospecific strategy from chiral pool material.