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[F] - 氟化物的捕获与释放:由鏻硼烷辅助的共沸干燥无亲核芳香族放射性氟化反应

[F]-Fluoride capture and release: azeotropic drying free nucleophilic aromatic radiofluorination assisted by a phosphonium borane.

作者信息

Perrio Cécile, Schmitt Sébastien, Pla Daniel, Gabbaï François P, Chansaenpak Kantapat, Mestre-Voegtle Béatrice, Gras Emmanuel

机构信息

Normandie Univ, UNICAEN, CEA, CNRS, UMR6301-ISTCT, LDM-TEP, Cyceron, Boulevard Henri Becquerel, 14000 Caen, France.

LCC, CNRS, UPR8241, UFTMP, 205, route de Narbonne, BP 44099, 31077 Toulouse Cedex 4, France.

出版信息

Chem Commun (Camb). 2016 Dec 22;53(2):340-343. doi: 10.1039/c6cc05168e.

Abstract

[F]-Fluoride ready for aromatic nucleophilic substitution was prepared according to a simple process including trapping of aqueous [F]-fluoride on a cartridge pre-loaded with the phosphonium borane [(PhMeP)CH(BMes)], then releasing by elution of TBACN in dry acetonitrile. Subsequent radiofluorination was successfully applied to a model reaction and to the radiosynthesis of [F]-setoperone.

摘要

用于芳香亲核取代反应的[F] - 氟化物是根据一个简单的过程制备的,该过程包括将水性[F] - 氟化物捕获在预先装载有硼烷鏻[(PhMeP)CH(BMes)]的柱上,然后通过在干燥乙腈中洗脱四丁基氯化铵(TBACN)来释放。随后,放射性氟化成功应用于模型反应和[F] - 司替戊醇的放射性合成。

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