The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 5-Amino-2-fluoropyridine(SMILESS: NC1=CN=C(C=C1)F,cas:1827-27-6) is researched.Computed Properties of C4H6N2O2S. The article 《Synthesis and in vitro evaluation of [18F]BMS-754807: A potential PET ligand for IGF-1R》 in relation to this compound, is published in Bioorganic & Medicinal Chemistry Letters. Let’s take a look at the latest research on this compound (cas:1827-27-6).
Radiosynthesis and in vitro evaluation of [18F](S)-1-(4-((5-cyclopropyl-1H-pyrazol-3-yl)amino)pyrrolo[2,1-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide ([18F]BMS-754807 or [18F] I) a specific IGF-1R inhibitor was performed. [18F]I demonstrated specific binding in vitro to human cancer tissues. Synthesis of reference standard II(X= F) and corresponding bromo derivative II(X = X = Br), the precursor for radiolabeling were achieved from 2,4-dichloropyrrolo[2,1-f][1,2,4]triazine in three steps with 50% overall yield. The radioproduct was obtained in 8% yield by reacting 1a with [18F]TBAF in DMSO at 170 °C at high radiochem. purity and specific activity (1-2 Ci/μmol, N = 10). The proof of concept of IGF-IR imaging with [18F]I was demonstrated by in vitro autoradiog. studies using pathol. identified surgically removed grade IV glioblastoma, breast cancer and pancreatic tumor tissues. These studies indicate that [18F]I can be a potential PET tracer for monitoring IGF-1R.
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