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The radiosynthesis of novel PI3K inhibitor , 8-ethoxy-2-(4-[(18) F]fluorophenyl)-3-nitro-2H-chromene ((18) F-EFPNC).
8-ethoxy-2-(4-[(18) F]fluorophenyl)-3-nitro-2H-chromene((18) F-EFPNC)was preparated through nucleophilic substitution reaction of the precursor 8-ethoxy -2-[(4 -N, N, N-trimethylammonium triflate)phenyl]-3-nitro-2H-chromene and nuclide [(18) F] fluorination. The best radiosynthesis condition was obtained via [(18) F] fluorination substitution reaction between [(18) F] and 18 mg of the precursor in dimethyl sulfoxide(DMSO) at 150 °C for 5 min after the radiosynthesis method was optimized.The decay-corrected radiochemical yields(DCRY) of (18) F-EFPNC were 38.5% with total synthesis time of 45 min.The radiochemical purity of (18) F-EFPNC was more than 95% by Thin-layer chromatography(TLC) analysis.The test of (18) F-EFPNC's radiochemical stability showed it was stable at room temperature for up to 2 h.The above results demonstrated that the radiosynthesis method of (18) F-EFPNC was feasible.
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