The Non-Anhydrous, Minimally Basic Synthesis of the Dopamine D2 Agonist [18F]MCL-524
Abstract
:1. Introduction
1.1. Aporphines
1.2. NAMB 18F Chemistry
1.3. Preperation of [18F]MCL-524
2. Materials and Methods
Radiosynthesis of [18F]MCL-524 ([18F]1) via In(OTf)3-Mediated Deprotection
3. Results
3.1. Summary of Non-Radioactive Synthesis
3.2. Summary of Radioactive Synthesis
4. Discussion
Supplementary Materials
Author Contributions
Funding
Data Availability Statement
Conflicts of Interest
References
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Entry | Reagent Added (Volume) | Time (min) | Temp (°C) | Conversion (%) a | DC-RCY (%) | Molar Activity b (GBq/µmol) |
---|---|---|---|---|---|---|
1 | 1:1 6 N H2SO4:MeOH (0.2 mL) | 5 | 100 | 5 | - c | - |
2 | 1:1 6 N H2SO4:MeOH (0.2 mL) | 10 | 150 | 86 | - c | - |
3 | In(OTf)3 d in H2O (0.1 mL) | 20 | 150 | 33, 35, 38 e | 6, 5, 9 e | 0.9, 0.7, 0.3 e |
4 | 90% TFA (1 mL) | 5 | 100 | 67 | 8 | 1.6 |
5 | 90% TFA (1 mL) | 10 | 100 | 83 | 14 | 2.0 |
6 | Yb(OTf)3 d·xH2O in H2O (0.1 mL) | 20 | 150 | 0 | - |
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Inkster, J.A.H.; Sromek, A.W.; Akurathi, V.; Neumeyer, J.L.; Packard, A.B. The Non-Anhydrous, Minimally Basic Synthesis of the Dopamine D2 Agonist [18F]MCL-524. Chemistry 2021, 3, 1047-1056. https://doi.org/10.3390/chemistry3030075
Inkster JAH, Sromek AW, Akurathi V, Neumeyer JL, Packard AB. The Non-Anhydrous, Minimally Basic Synthesis of the Dopamine D2 Agonist [18F]MCL-524. Chemistry. 2021; 3(3):1047-1056. https://doi.org/10.3390/chemistry3030075
Chicago/Turabian StyleInkster, James A. H., Anna W. Sromek, Vamsidhar Akurathi, John L. Neumeyer, and Alan B. Packard. 2021. "The Non-Anhydrous, Minimally Basic Synthesis of the Dopamine D2 Agonist [18F]MCL-524" Chemistry 3, no. 3: 1047-1056. https://doi.org/10.3390/chemistry3030075