4-Amino-1-Boc-piperidine is utilized as a versatile starting material in organic synthesis, enabling the preparation of various bioactive compounds with pharmaceutical relevance. It serves as a key intermediate in the synthesis of N-(3-(4-hydroxyphenyl)-propenoyl)-amino acid tryptamides, which act as inhibitors of the silent information regulator human type 2 (SIRT2) enzyme. Additionally, it is employed in the synthesis of piperidine-substituted triazine derivatives and piperidinylamino-diarylpyrimidine (pDAPY) derivatives, which exhibit potent activity as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs). Moreover, 4-Amino-1-Boc-piperidine plays a crucial role in the microwave-assisted solid-phase synthesis of N-substituted piperidines via direct annulation of primary amines with resin-bound dimesylates. This compound's versatility and reactivity make it a valuable tool in medicinal chemistry and drug discovery efforts, offering potential applications in the treatment of various diseases, including HIV infection.