166173-78-0Relevant articles and documents
Optimization of 18F-syntheses using 19F-reagents at tracer-level concentrations and liquid chromatography/tandem mass spectrometry analysis: Improved synthesis of [18F]MDL100907
Zhang, Xiang,Dunlow, Ryan,Blackman, Burchelle N.,Swenson, Rolf E.
, p. 427 - 437 (2018/04/30)
Traditional radiosynthetic optimization faces the challenges of high radiation exposure, cost, and inability to perform serial reactions due to tracer decay. To accelerate tracer development, we have developed a strategy to simulate radioactive 18F-syntheses by using tracer-level (nanomolar) non-radioactive 19F-reagents and LC-MS/MS analysis. The methodology was validated with fallypride synthesis under tracer-level 19F-conditions, which showed reproducible and comparable results with radiosynthesis, and proved the feasibility of this process. Using this approach, the synthesis of [18F]MDL100907 was optimized under 19F-conditions with greatly improved yield. The best conditions were successfully transferred to radiosynthesis. A radiochemical yield of 19% to 22% was achieved with the radiochemical purity >99% and the molar activity 38.8 to 53.6?GBq/ μmol (n?=?3). The tracer-level 19F-approach provides a high-throughput and cost-effective process to optimize radiosynthesis with reduced radiation exposure. This new method allows medicinal and synthetic chemists to optimize radiolabeling conditions without the need to use radioactivity.
A new multi-gram synthetic route to labeling precursors for the D2/3 PET agent 18F-fallypride
Kim, Kwangho,Miller, Nicole R.,Sulikowski, Gary A.,Lindsley, Craig W.
scheme or table, p. 4467 - 4469 (2009/04/06)
This Letter describes a new multi-gram synthetic protocol for the preparation of the classic tosylate labeling precursor for the D2/3 PET agent [18F]fallypride. In the course of our studies, we also discovered two novel labeling prec
In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D2-like dopamine receptors
Stark, Daniela,Piel, Markus,Huebner, Harald,Gmeiner, Peter,Gruender, Gerhard,Roesch, Frank
, p. 6819 - 6829 (2008/03/27)
Benzamide derivatives as radiotracers have played an important role in diagnosing malfunction in dopaminergic neurotransmission. A variety of halogenated and two unsubstituted benzamide derivatives were synthesised and their in vitro affinities to dopaminergic, serotonergic and adrenergic receptors and their lipophilicities were determined. As references IBZM (3), raclopride (4) and FLB457 (5) were tested as well. The two iodinated compounds NAE (27) and NADE (28) displayed Ki values of 0.68 and 14 nM for the D2 receptor. The well-established radiotracers FP (1) and DMFP (2) showed affinities in the same range as did the brominated compounds NABrE (29) and NABrDE (30). The log D7.4 values of 2.91 for NAE (27) and of 2.81 for NADE (28) are in the range of those found for IBZM (3), FP (1) and DMFP (2). These facts allow to expect good properties for the two iodinated compounds NAE (27) and NADE (28) regarding in vivo imaging with SPECT.