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We report methods for the synthesis of vertex-differentiated icosahedral closo-boranes. A single B-OH vertex of the icosahedral borane [closo-B(12)(OH)(12)](2-) was derivatized to prepare [closo-B(12)(OR)(OH)(11)](2-) using optimized alkylation conditions and purification procedures. Several representative vertex-differentiated icosahedral closo-boranes were prepared utilizing carbonate ester and azide-alkyne click chemistries on the surface of the closo-B(12)(2-) core.

Synthesis of Vertex-Differentiated Icosahedral closo-Boranes: Polyfunctional Scaffolds for Targeted Drug Delivery