Boc-Leucinol is widely used in organic synthesis, particularly in the development of pharmaceuticals and peptide-based compounds. It serves as a protected amino alcohol building block, enabling controlled assembly of complex molecules without unwanted side reactions. Its Boc (tert-butoxycarbonyl) group provides temporary protection of the amine functionality, allowing selective reactions at other sites, which is essential in stepwise peptide synthesis.

It is commonly employed in the preparation of protease inhibitors, receptor agonists, and enzyme modulators due to its structural similarity to natural amino acid derivatives. The leucinol backbone contributes chirality and favorable steric properties, enhancing stereoselectivity in asymmetric synthesis. Additionally, Boc-Leucinol is used in solid-phase synthesis and combinatorial chemistry for generating libraries of bioactive molecules. Its stability and ease of deprotection make it a preferred intermediate in drug discovery and medicinal chemistry workflows.