Macrocycloadditions leading to conformationally restricted small molecules.
[reaction: see text] The Cu(I)-catalyzed cycloaddition of alkynes and azides (click reaction) provides a robust method for the construction of macrocyclic small molecules via an intramolecular macrocycloaddition. A three-subunit system has been used to explore the tolerance of this macrocycloaddition to variations of stereochemistries and substituents.
Looper
Ryan E
RE
Howard Hughes Medical Institute, Department of Chemistry and Chemical Biology, Harvard University, Broad Institute of Harvard and MIT, Cambridge, Massachusetts 02138, USA.
Pizzirani
Daniela
D
Schreiber
Stuart L
SL