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Syntheses of no‐carrier‐added (NCA) [ 18 F]fluoroalkyl halides and their application in the syntheses of [ 18 F]fluoroalkyl derivatives of neurotransmitter receptor active compounds
Author(s) -
Shiue C.Y.,
Bai L.Q.,
Teng R.R.,
Wolf A. P.
Publication year - 1987
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580240108
Subject(s) - chemistry , halide , yield (engineering) , reagent , alkylation , nucleophilic substitution , alkyl , medicinal chemistry , nucleophile , organic chemistry , materials science , metallurgy , catalysis
Nucleophilic aliphatic substitution of alkyl halides, 1 , [(CH 2 ) n X 2 (n=2, 3; X=Br,I)], with NCA K[ 18 F]/Kryptofix 2.2.2 in CH 3 CN gave the corresponding NCA [ 18 F]fluoroalkyl halides 2 in 30–40% yields. The factors which influence the yield of 2 were compared. N ‐Alkylation of several neurotransmitter receptor active amides and amines with this reagent gave the corresponding NCA N ‐[ 18 F]fluoroalkyl derivatives ( 3–6 ) in 20–60% yield.