Boc-D-Valinol is widely used in organic synthesis, particularly in the pharmaceutical and medicinal chemistry fields. Its primary application lies in the construction of complex peptides and peptidomimetics, where the Boc (tert-butyloxycarbonyl) protecting group ensures selective reactivity of the amine functionality during stepwise assembly. The D-Valinol backbone provides a chiral, non-natural amino alcohol structure that is valuable in designing enzyme inhibitors or bioactive molecules with enhanced metabolic stability.

It serves as a key intermediate in the synthesis of active pharmaceutical ingredients (APIs), especially in drugs targeting central nervous system disorders, protease inhibitors, and anticancer agents. The stereochemistry of the D-configuration is crucial for achieving desired biological activity and resistance to enzymatic degradation in vivo.

Additionally, Boc-D-Valinol is employed in asymmetric synthesis and catalysis, where its hydroxyl and protected amine groups allow for selective transformations and the formation of heterocyclic compounds. Its compatibility with solid-phase synthesis and various coupling reagents makes it a preferred building block in combinatorial chemistry and drug discovery research.