H. Manning
Faculty Member
Last active: 3/22/2018

Microwave-assisted Organic Synthesis of a High-affinity Pyrazolo-pyrimidinyl TSPO Ligand.

Tang D, Buck JR, Hight MR, Manning HC
Tetrahedron Lett. 2010 51 (35): 4595-4598

PMID: 20689673 · PMCID: PMC2913893 · DOI:10.1016/j.tetlet.2010.06.074

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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