Stereospecific Synthesis of Substituted Sulfamidates as Privileged Morpholine Building Blocks

Autor: Chiara Borsari, Matthias P. Wymann, Pierre Boulay, Claudio Meyer, Uros Stojiljkovic, Paul Hebeisen, Denise Rageot
Rok vydání: 2022
Předmět:
Zdroj: Synthesis. 55:499-509
ISSN: 1437-210X
0039-7881
Popis: 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.
Databáze: OpenAIRE