Diversity-Oriented Synthesis of Morpholine-Containing Molecular Scaffolds

Couple and cyclize: A coupling–cyclization strategy employing building blocks from the chiral pool was applied for the generation of morpholine-containing scaffolds (see scheme). The modulation of both the reaction conditions and the stereochemistry of the building blocks allowed the first degree of skeletal diversity, followed by functional group pairing of strategic appendages of selected molecular scaffolds to achieve more complex molecular frameworks.