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Microwave-assisted organic synthesis of a high-affinity pyrazolo-pyrimidinyl TSPO ligand |
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| Authors: | Dewei Tang Jason R. Buck Matthew R. Hight H. Charles Manning |
| Affiliation: | a Vanderbilt University Institute of Imaging Science, Nashville, TN 37232, USA b Program in Chemical and Physical Biology, Vanderbilt University, Nashville, TN 37232, USA c Department of Radiology and Radiological Science, Vanderbilt University Medical Center, Nashville, TN 37232, USA d Department of Physics and Astronomy, Program in Materials Science, Vanderbilt University, Nashville, TN 37235, USA e Department of Biomedical Imaging, Vanderbilt University, Nashville, TN 37235, USA f Department of Neurosurgery, Vanderbilt University Medical Center, Nashville, TN 37232, USA g Vanderbilt Ingram Cancer Center(VICC), Vanderbilt University Medical Center, Nashville, TN 37232, USA |
| Abstract: | We herein report a dramatically improved total synthesis of the high-affinity translocator protein (TSPO) ligand DPA-714, featuring microwave-assisted organic synthesis (MAOS). Compared with previously described approaches, our novel MAOS method dramatically reduces overall reaction time without adversely effecting reaction yields. We envision that the described MAOS protocol may be suitably applied to high-throughput, diversity-oriented synthesis of novel compounds based on the pyrazolo-pyrimidinyl scaffold. Such an approach could accelerate the development of focused libraries of novel TSPO ligands with potential for future development as molecular imaging and therapeutic agents. |
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