4.5 Article

Stereospecific Synthesis of Substituted Sulfamidates as Privileged Morpholine Building Blocks

Journal

SYNTHESIS-STUTTGART
Volume 55, Issue 3, Pages 499-509

Publisher

GEORG THIEME VERLAG KG
DOI: 10.1055/a-1915-7794

Keywords

morpholines; sulfamidates; stereoselectivity; chiral building blocks; privileged scaffolds

Ask authors/readers for more resources

In this study, a method for synthesizing optically pure morpholine building blocks from chiral pool material is reported, which is of great significance for improving the properties of active pharmaceutical ingredients.
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.

Authors

I am an author on this paper
Click your name to claim this paper and add it to your profile.

Reviews

Primary Rating

4.5
Not enough ratings

Secondary Ratings

Novelty
-
Significance
-
Scientific rigor
-
Rate this paper

Recommended

No Data Available
No Data Available