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. 2015 May 1;25(9):1965-70.
doi: 10.1016/j.bmcl.2015.03.021. Epub 2015 Mar 14.

Synthesis of [(11)C]GSK1482160 as a new PET agent for targeting P2X(7) receptor

Mingzhang Gao  1 , Min Wang  1 , Mark A Green  1 , Gary D Hutchins  1 , Qi-Huang Zheng  2
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Free article

Synthesis of [(11)C]GSK1482160 as a new PET agent for targeting P2X(7) receptor

Mingzhang Gao et al. Bioorg Med Chem Lett. .
Free article

Abstract

The authentic standards GSK1482160 and its isomer, as well as the radiolabeling precursors desmethyl-GSK1482160 and Boc-protected desmethyl-GSK1482160 were synthesized from L-pyroglutamic acid, methyl L-pyroglutamate and 2-chloro-3-(trifluoromethyl)benzylamine with overall chemical yield 27-28% in 3 steps, 58% in 4 steps, 76% in 1 step and 33% in 2 steps, respectively. [(11)C]GSK1482160 was prepared from either desmethyl-GSK1482160 or Boc-protected desmethyl-GSK1482160 with [(11)C]CH3OTf through N-[(11)C]methylation and isolated by HPLC combined with SPE in 40-50% and 30-40% radiochemical yield, respectively, based on [(11)C]CO2 and decay corrected to end of bombardment (EOB). The radiochemical purity was >99%, and the specific activity at EOB was 370-1110 GBq/μmol with a total synthesis time of ∼40-min from EOB.

Keywords: Neuroinflammation; P2X(7) receptor; Positron emission tomography (PET); Radiosynthesis; [(11)C]GSK1482160.

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