Morpholine is a heterocyclic moiety that is 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 the synthesis of optically pure 3-hydroxymethylmorpholine building blocks, as well as their sulfamidates, exploiting a stereospecific strategy from chiral pool material.
Stereospecific Synthesis of Substituted Sulfamidates as Privileged Morpholine Building Blocks / U. Stojiljkovic, C. Meyer, P. Boulay, P. Hebeisen, D. Rageot, M.P. Wymann, C. Borsari. - In: SYNTHESIS. - ISSN 0039-7881. - 55:3(2023 Feb 02), pp. 499-509. [10.1055/a-1915-7794]
Stereospecific Synthesis of Substituted Sulfamidates as Privileged Morpholine Building Blocks
C. Borsari
Ultimo
2023
Abstract
Morpholine is a heterocyclic moiety that is 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 the synthesis of optically pure 3-hydroxymethylmorpholine building blocks, as well as their sulfamidates, exploiting a stereospecific strategy from chiral pool material.File | Dimensione | Formato | |
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