| Literature DB >> 25819093 |
Mingzhang Gao1, Min Wang1, Mark A Green1, Gary D Hutchins1, Qi-Huang Zheng2.
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.Entities:
Keywords: Neuroinflammation; P2X(7) receptor; Positron emission tomography (PET); Radiosynthesis; [(11)C]GSK1482160
Mesh：
Substances：
Year: 2015 PMID： 25819093 DOI： 10.1016/j.bmcl.2015.03.021
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823