Multicomponent Macrocyclization Reactions (MCMRs) Employing Highly Reactive Acyl Ketene and Nitrile Oxide Intermediates

Bidirectional macrocyclization of peptides by double multicomponent reactions.

Increasing the diversity of peptide cyclization methods is an effective way of accessing new types of macrocyclic chemotypes featuring a wide variety of ring sizes and topologies. Multicomponent reactions (MCRs) are processes capable of generating great levels of molecular diversity and complexity at low synthetic cost. In an attempt to further exploit MCRs in the field of cyclopeptides, we des...

Aldol type Condensation Reactions of Acyl Ketene Dithioacetals

Highly regioselective nitrile oxide dipolar cycloadditions with ortho-nitrophenyl alkynes.

The dipolar cycloadditions of ortho-nitrophenyl alkynes with aryl nitrile oxides has been demonstrated. A range of substituents are tolerated on the alkyne. These reactions proceed with excellent levels of regioselectivity. Subsequent functionalization of the isoxazole scaffold has been demonstrated.

Multicomponent Reactions

Multicomponent reactions

Chemistry as a central science is facing a steadily increasing demand for new chemical entities (NCE). Innovative solutions, in all kinds of disciplines that depend on chemistry, require new molecules with specific properties, and their societal consequences are fundamental and pioneering. However, NCE not only demand a realistic structural space but also their feasibility poses challenges to s...