Rapid synthesis of F??18 and H??2 dual??labeled altanserin, a metabolically resistant PET ligand for 5??HT2a receptors

…, RM Baldwin, T Fu, DS Charney…

Index: Tan, Ping-Zhong; Baldwin, Ronald M.; Fu, Tao; Charney, Dennis S.; Innis, Robert B. Journal of Labelled Compounds and Radiopharmaceuticals, 1999 , vol. 42, # 5 p. 457 - 467

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Citation Number: 26

Abstract

Abstract F-18 and H-2 dual-labeled altanserin (3,[18 F] d-ALT), a novel PET tracer for 5-HT 2A receptors with metabolically resistant properties, was synthesized by [18 F] fluoride displacement of the corresponding deuterated nitro precursor in 32% yield (EOB) in 108 min with radiochemical purity 95% and specific activity> 1000 mCi/μmol (EOS). The key intermediate ethyl N-(2-chloroethyl-2, 2-d 2) carbamate (7) was obtained by LiA1D 4 ...