You need JavaScript to view this

A facile and rapid automated synthesis of 3'-deoxy-3'-[{sup 18}F]fluorothymidine

Abstract

Aim: To develop a simplified and fully automated synthesis procedure of 3'-deoxy-3'-[{sup 18}F]fluorothymidine ([{sup 18}F]FLT) using PET-MF-2V-IT-I synthesis module. Methods: Synthesis of [{sup 18}F]FLT was performed using PET-MF-2V-IT-I synthesis module by one-pot two-step reaction procedure, including nucleophilic fluorination of 3-N-t-butoxycarbonyl-1-[5'-O-(4,4'-dimethoxy triphenylmethyl)-2'-deoxy-3'-O-(4-nitrobenzenesulfonyl) -{beta}-D-threopentofuranosyl]thymine (15 mg) as the precursor molecule with [{sup 18}F]fluoride, and subsequent hydrolysis of the protecting group with 1.0 M HCl at the same reaction vessel and purification with SEP PAK cartridges instead of the HPLC system. Results: The automated synthesis of [{sup 18}F]FLT with SEP PAK purification gave corrected radiochemical yield of 23.2{+-}2.6% (n=6, uncorrected yield: 16-22%) and radiochemical purity of >97% within the total synthesis time of 35 min. Conclusion: The fully one-pot automated synthesis procedure with SEP PAK purification can be applied to the fully automated synthesis of [{sup 18}F]FLT using commercial [{sup 18}F]FDG synthesis module.
Authors:
Tang Ganghua, E-mail: gtang0224@yahoo.com.c [PET-CT Center, Department of Nuclear Medicine, The First Affiliated Hospital, Sun Yat-Sen University, Guangzhou 510080 (China); Nan Fang PET Center, Nan Fang Hospital, Southern Medical University, Guangzhou 510515 (China)]; Xiaolan, Tang; [1]  Fuhua, Wen; [2]  Mingfang, Wang; Baoyuan, Li [3] 
  1. College of Science, South China Agricultural University, Guangzhou 510642 (China)
  2. PET-CT Center, Department of Nuclear Medicine, The First Affiliated Hospital, Sun Yat-Sen University, Guangzhou 510080 (China)
  3. Nan Fang PET Center, Nan Fang Hospital, Southern Medical University, Guangzhou 510515 (China)
Publication Date:
Sep 15, 2010
Product Type:
Journal Article
Resource Relation:
Journal Name: Applied Radiation and Isotopes; Journal Volume: 68; Journal Issue: 9; Other Information: DOI: 10.1016/j.apradiso.2010.04.010; PII: S0969-8043(10)00153-3; Copyright (c) 2010 Elsevier Science B.V., Amsterdam, The Netherlands, All rights reserved.
Subject:
07 ISOTOPES AND RADIATION SOURCES; FLUORIDES; FLUORINATION; FLUORINE 18; HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY; HYDROCHLORIC ACID; HYDROLYSIS; PRECURSOR; PURIFICATION; RADIOPHARMACEUTICALS; SYNTHESIS; BETA DECAY RADIOISOTOPES; BETA-PLUS DECAY RADIOISOTOPES; CHEMICAL REACTIONS; CHLORINE COMPOUNDS; CHROMATOGRAPHY; DECOMPOSITION; DRUGS; FLUORINE COMPOUNDS; FLUORINE ISOTOPES; HALIDES; HALOGEN COMPOUNDS; HALOGENATION; HOURS LIVING RADIOISOTOPES; HYDROGEN COMPOUNDS; INORGANIC ACIDS; INORGANIC COMPOUNDS; ISOMERIC TRANSITION ISOTOPES; ISOTOPES; LABELLED COMPOUNDS; LIGHT NUCLEI; LIQUID COLUMN CHROMATOGRAPHY; LYSIS; MATERIALS; NANOSECONDS LIVING RADIOISOTOPES; NUCLEI; ODD-ODD NUCLEI; RADIOACTIVE MATERIALS; RADIOISOTOPES; SEPARATION PROCESSES; SOLVOLYSIS
OSTI ID:
21418577
Country of Origin:
United Kingdom
Language:
English
Other Identifying Numbers:
Journal ID: ISSN 0969-8043; ARISEF; TRN: GB10R4462012719
Availability:
Available from http://dx.doi.org/10.1016/j.apradiso.2010.04.010
Submitting Site:
GBN
Size:
page(s) 1734-1739
Announcement Date:
May 05, 2011

Citation Formats

Tang Ganghua, E-mail: gtang0224@yahoo.com.c [PET-CT Center, Department of Nuclear Medicine, The First Affiliated Hospital, Sun Yat-Sen University, Guangzhou 510080 (China), Nan Fang PET Center, Nan Fang Hospital, Southern Medical University, Guangzhou 510515 (China)], Xiaolan, Tang, Fuhua, Wen, Mingfang, Wang, and Baoyuan, Li. A facile and rapid automated synthesis of 3'-deoxy-3'-[{sup 18}F]fluorothymidine. United Kingdom: N. p., 2010. Web. doi:10.1016/j.apradiso.2010.04.010.
Tang Ganghua, E-mail: gtang0224@yahoo.com.c [PET-CT Center, Department of Nuclear Medicine, The First Affiliated Hospital, Sun Yat-Sen University, Guangzhou 510080 (China), Nan Fang PET Center, Nan Fang Hospital, Southern Medical University, Guangzhou 510515 (China)], Xiaolan, Tang, Fuhua, Wen, Mingfang, Wang, & Baoyuan, Li. A facile and rapid automated synthesis of 3'-deoxy-3'-[{sup 18}F]fluorothymidine. United Kingdom. https://doi.org/10.1016/j.apradiso.2010.04.010
Tang Ganghua, E-mail: gtang0224@yahoo.com.c [PET-CT Center, Department of Nuclear Medicine, The First Affiliated Hospital, Sun Yat-Sen University, Guangzhou 510080 (China), Nan Fang PET Center, Nan Fang Hospital, Southern Medical University, Guangzhou 510515 (China)], Xiaolan, Tang, Fuhua, Wen, Mingfang, Wang, and Baoyuan, Li. 2010. "A facile and rapid automated synthesis of 3'-deoxy-3'-[{sup 18}F]fluorothymidine." United Kingdom. https://doi.org/10.1016/j.apradiso.2010.04.010.
@misc{etde_21418577,
title = {A facile and rapid automated synthesis of 3'-deoxy-3'-[{sup 18}F]fluorothymidine}
author = {Tang Ganghua, E-mail: gtang0224@yahoo.com.c [PET-CT Center, Department of Nuclear Medicine, The First Affiliated Hospital, Sun Yat-Sen University, Guangzhou 510080 (China), Nan Fang PET Center, Nan Fang Hospital, Southern Medical University, Guangzhou 510515 (China)], Xiaolan, Tang, Fuhua, Wen, Mingfang, Wang, and Baoyuan, Li}
abstractNote = {Aim: To develop a simplified and fully automated synthesis procedure of 3'-deoxy-3'-[{sup 18}F]fluorothymidine ([{sup 18}F]FLT) using PET-MF-2V-IT-I synthesis module. Methods: Synthesis of [{sup 18}F]FLT was performed using PET-MF-2V-IT-I synthesis module by one-pot two-step reaction procedure, including nucleophilic fluorination of 3-N-t-butoxycarbonyl-1-[5'-O-(4,4'-dimethoxy triphenylmethyl)-2'-deoxy-3'-O-(4-nitrobenzenesulfonyl) -{beta}-D-threopentofuranosyl]thymine (15 mg) as the precursor molecule with [{sup 18}F]fluoride, and subsequent hydrolysis of the protecting group with 1.0 M HCl at the same reaction vessel and purification with SEP PAK cartridges instead of the HPLC system. Results: The automated synthesis of [{sup 18}F]FLT with SEP PAK purification gave corrected radiochemical yield of 23.2{+-}2.6% (n=6, uncorrected yield: 16-22%) and radiochemical purity of >97% within the total synthesis time of 35 min. Conclusion: The fully one-pot automated synthesis procedure with SEP PAK purification can be applied to the fully automated synthesis of [{sup 18}F]FLT using commercial [{sup 18}F]FDG synthesis module.}
doi = {10.1016/j.apradiso.2010.04.010}
journal = []
issue = {9}
volume = {68}
place = {United Kingdom}
year = {2010}
month = {Sep}
}