A one-step automated high-radiochemical-yield synthesis of 18F-FECNT from mesylate precursor.
2Beta-carbomethoxy-3beta-(4-chlorophenyl)-8-(2-[(18)F]fluoroethyl)nortropane ((18)F-FECNT) is a potential dopamine transporter imaging agent. In this article, a new mesylate precursor was prepared and a one-step automated synthesis of (18)F-FECNT was developed. The mesylate precursor (4) was synthesized from 2beta-carbomethoxy-3beta-(4-chlorophenyl)tropane (1) by N-demethylation, hydroxyethylation followed by mesylation at a total yield of 47%. [(18)F]fluorination was performed by heating 4mg mesylate precursor and K[(18)F] in 1 ml acetonitrile at 90 degrees C for 20 min. The crude (18)F-FECNT was obtained with a radiolabeling yield of 48%. After purification by preparative high performance liquid chromatography (HPLC), the final (18)F-FECNT product was obtained with a radiochemical purity of 98.4% and a decay corrected radiochemical yield of 33+/-9% (and the uncorrected radiochemical yield was 19+/-5%, n=5). The duration of the total procedure was 80-90 min.
Chen
Zheng Ping
ZP
School of Medicine and Pharmaceutics, Jiangnan University, Wuxi, PR China.
Wang
Song Pei
SP
Li
Xiao Min
XM
Liu
Chun Yi
CY
Tang
Jie
J
Cao
Guo Xian
GX
Luo
Shi Neng
SN
Zhang
Lian Fen
LF
Jin
Jian
J
D007553:Isotope Labeling / Q000295:instrumentation*; D008698:Mesylates / Q000737:chemistry*; D009662:Nortropanes / Q000737:chemistry* / Q000302:isolation & purification*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000302:isolation & purification*; D012371:Robotics / Q000295:instrumentation*
C410211:2-carbomethoxy-3-(4-chlorophenyl)-8-(2-fluoroethyl)nortropane; D008698:Mesylates; D009662:Nortropanes; D019275:Radiopharmaceuticals