An improved, regioselective synthesis of the radiolabelling precursor for the translocator protein targeting positron emission tomography imaging radiotracer [F-18]GE-180

作者：Morisson Iveson Veronique; Wadsworth Harry; Passmore Joanna; Ewan Amanda; Nilsen Sondre; Thaning Mikkel; Trigg William^*

来源：Tetrahedron Letters, 2014, 55(37): 5141-5143.

DOI：10.1016/j.tetlet.2014.07.090

• Positron emission tomography
• Target translocator protein
• Indole
• Regioselectivity
• GE-180

[F-18]GE-180 has been demonstrated to be a promising new positron emission tomography radiotracer for targeting translocator protein. PET imaging of TSPO will enable measurement of neuroinflammation and microglia activity in vivo. The synthetic route used in the initial discovery of GE-180, whilst enabling the rapid evaluation of the structure-activity relationships (SAR) in this molecular class, was not high yielding and not suitable for scale-up. Here we present an optimised route towards GE-180 and the radiolabelling precursor of [F-18]GE-180 with significantly improved yields due to a strategy which improves the regioselectivity of the key indole formation step of the synthesis.

• 出版日期2014-9-10