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“The biggest stumbling block for biological sciences turned out to be synthetic organic chemistry” – Elias A. Zerhouni, Former NIH Director in Chemical & Engineering News, July 3, 2008. The above statement signifies the importance of organic synthesis in today's modern era of scientific research, aimed towards the betterment of human life. The Core Synthesis Facility at North Dakota State University was established as a part of the Center for Protease Research in April 2008, with funding from an NCRR-NIH-COBRE grant. The primary objective of the facility is to act as a strong in-house support system, to facilitate biomedical researchers in accomplishing their research goals. The Core Synthesis Facility is equipped with modern synthetic technologies and state of the art instrumentation. The research in the facility is focused on organic synthesis of small molecules for biomedical applications and analytical characterization of substrates of interest. The past and current research projects involve synthesis of enzyme inhibitors/activators, fluorescent labeling of amino acids and quantitative/qualitative analysis by HPLC. We also offer scientific consultation and provide student training. On a whole, the research at the Core Synthesis Facility is dedicated towards the treatment of a variety of diseases, thereby bridging the gap between chemistry and biology.