Département de chimie moléculaire

The access to multifunctional biomol. compds. involves multistep reactions usually with a complicated protection scheme and lengthy sepn. processes. The development of a strategy combining several orthogonal ligations is highly desirable. Herein, the authors introduce a new method that involves two orthogonal copper-mediated ligations of azide with alkyne, and amine with thioacid. The authors established compatible conditions to carry out mol. assemblies of three different chem. components in a single one-pot reaction. The effectiveness of the method was demonstrated in the synthesis of biomol. compds. that are known to target tumor tissue. The simple reaction conditions suggest that this strategy of combining several orthogonal ligations could have wide potential for the chem. synthesis of complex macromols. [on SciFinder(R)]