Fully automated synthesis of PET TSPO radioligands [11C]DAA1106 and [18F]FEDAA1106
Creators
- 1. Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, L3-208, Indianapolis, IN 46202-2111 (United States)
Description
[11C]DAA1106 was prepared by O-[11C]methylation of DAA1123 with [11C]CH3OTf and NaH in CH3CN at 80 °C and isolated by HPLC combined with SPE purification in 60–70% decay corrected radiochemical yield. [18F]FEDAA1106 was synthesized by the nucleophilic substitution of tosyloxy-FEDAA1106 in DMSO with K[18F]F/Kryptofix 2.2.2 at 140 °C and isolated by HPLC combined with SPE purification in 30–60% decay corrected radiochemical yield. The specific activity for [11C]DAA1106 and [18F]FEDAA1106 was 370–740 GBq/μmol and 37–222 GBq/μmol at EOB, respectively. - Highlights: ► Fully automated syntheses of [11C]DAA1106 and [18F]FEDAA1106 have been developed. ► Simplified solid-phase extraction (SPE) method was employed in radiosynthesis. ► Syntheses of DAA1106, FEDAA1106 and their precursors have been improved.
Availability note (English)
Available from http://dx.doi.org/10.1016/j.apradiso.2012.03.011Additional details
Identifiers
- DOI
- 10.1016/j.apradiso.2012.03.011;
- PII
- S0969-8043(12)00212-6;
Publishing Information
- Journal Title
- Applied Radiation and Isotopes
- Journal Volume
- 70
- Journal Issue
- 6
- Journal Page Range
- p. 965-973
- ISSN
- 0969-8043
- CODEN
- ARISEF
INIS
- Country of Publication
- United Kingdom
- Country of Input or Organization
- International Atomic Energy Agency (IAEA)
- INIS RN
- 43073015
- Subject category
- S07: ISOTOPES AND RADIATION SOURCES;
- Descriptors DEI
- ACETONITRILE; CARBON 11; DMSO; EXTRACTION; FLUORINE 18; HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY; ISOTOPE PRODUCTION; METHYLATION; POSITRON COMPUTED TOMOGRAPHY; PURIFICATION; SYNTHESIS
- Descriptors DEC
- BETA DECAY RADIOISOTOPES; BETA-PLUS DECAY RADIOISOTOPES; CARBON ISOTOPES; CHEMICAL REACTIONS; CHROMATOGRAPHY; COMPUTERIZED TOMOGRAPHY; DIAGNOSTIC TECHNIQUES; EMISSION COMPUTED TOMOGRAPHY; EVEN-ODD NUCLEI; FLUORINE ISOTOPES; HOURS LIVING RADIOISOTOPES; ISOMERIC TRANSITION ISOTOPES; ISOTOPES; LIGHT NUCLEI; LIQUID COLUMN CHROMATOGRAPHY; MINUTES LIVING RADIOISOTOPES; NANOSECONDS LIVING RADIOISOTOPES; NITRILES; NUCLEI; ODD-ODD NUCLEI; ORGANIC COMPOUNDS; ORGANIC NITROGEN COMPOUNDS; ORGANIC SULFUR COMPOUNDS; RADIOISOTOPES; SEPARATION PROCESSES; SULFOXIDES; TOMOGRAPHY
Optional Information
- Copyright
- Copyright (c) 2012 Elsevier Science B.V., Amsterdam, The Netherlands, All rights reserved.