On December 1, 2019, Wu, Renbo; Liu, Song; Liu, Yajing; Sun, Yuli; Cheng, Xuebo; Huang, Yong; Yang, Zequn; Wu, Zehui published an article.Synthetic Route of 98946-18-0 The title of the article was Synthesis and biological evaluation of [18F](2S,4S)4-(3-fluoropropyl) arginine as a tumor imaging agent. And the article contained the following:
Designing novel 18F-labeled amino acid derivatives for targeted amino acid transporters is an attractive strategy for the development of therapeutic and diagnostic agents for cancer therapy. In this work, we have developed a novel 3-fluoropropyl analog of arginine, namely, (2S,4S)4-[18F]FPArg, [18F]1, to be used as a probe for studying arginine metabolism Optically pure and labeled with 18F and 19F, (2S,4S)4-(3-fluoropropyl)arginine was synthesized and isolated in high radiochem. purity (>95%). In vitro uptake assays in human MCF-7 cells revealed that [18F]1 enters cells mainly via sodium-independent cationic amino acid transporters and was inhibited >62% by arginine. [18F]1 showed a high cellular uptake of 7.3 ± 0.24% and 6.07 ± 0.3% uptake/100 mg protein after incubation in MCF-7 and MDA-MB-231 cells for 120 min, resp. In vivo biodistribution studies demonstrated that [18F]1 provided high tumor uptake and high tumor to muscle ratios (5:1 at the 30 and 60 min time points). In vivo PET imaging studies demonstrated tumor-specific uptake in nude mice bearing MCF-7 breast tumors with an excellent tumor-to-muscle ratio. These results suggest that [18F]1 is a promising tracer for clin. breast cancer imaging and may be used to diagnose and monitor diseases that are associated with arginine metabolism The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Synthetic Route of 98946-18-0
The Article related to fluoropropyl arginine 18f isotope synthesis tumor imaging agent pet, amino acid uptake breast tumor biodistribution metabolism diagnostic agent, pyrazole carboxamidine guanidinylation mitsunobu reaction protection coupling fluorination reduction, phase transfer catalyst steric hindrance, arginine, breast cancer, cationic amino acid transporter and other aspects.Synthetic Route of 98946-18-0
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