Strained Ammonium Precursors for Radiofluorinations
Abstract The increasing application of positron emission tomography (PET) in nuclear medicine has stimulated the extensive development of a multitude of novel and versatile techniques to introduce fluorine‐18, especially for the radiolabelling of biologically or pharmacologically active molecules. T...
| Main Authors: | , |
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| Format: | Article |
| Language: | English |
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Wiley-VCH
2022-06-01
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| Series: | ChemistryOpen |
| Subjects: | |
| Online Access: | https://doi.org/10.1002/open.202200039 |
| _version_ | 1811344410296713216 |
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| author | Dr. Falco Reissig Dr. Constantin Mamat |
| author_facet | Dr. Falco Reissig Dr. Constantin Mamat |
| author_sort | Dr. Falco Reissig |
| collection | DOAJ |
| description | Abstract The increasing application of positron emission tomography (PET) in nuclear medicine has stimulated the extensive development of a multitude of novel and versatile techniques to introduce fluorine‐18, especially for the radiolabelling of biologically or pharmacologically active molecules. Taking into consideration that the introduction of fluorine‐18 (t1/2=109.8 min) mostly proceeds under harsh conditions, radiolabelling of such molecules represents a challenge and is of enormous interest. Ideally, it should proceed in a regioselective manner under mild physiological conditions, in an acceptable time span, with high yields and high specific activities. Special attention has been drawn to 2‐fluoroethyl and 3‐fluoropropyl groups, which are often the active sites of radiofluorinated compounds. Precursors containing an ammonium leaving group – such as a strained azetidinium or aziridinium moiety – can help to overcome these obstacles leading to a convenient and mild introduction of [18F]fluoride with high radiochemical yields. |
| first_indexed | 2024-04-13T19:46:54Z |
| format | Article |
| id | doaj.art-117d498d16cb40f8bce3afa9019de83e |
| institution | Directory Open Access Journal |
| issn | 2191-1363 |
| language | English |
| last_indexed | 2024-04-13T19:46:54Z |
| publishDate | 2022-06-01 |
| publisher | Wiley-VCH |
| record_format | Article |
| series | ChemistryOpen |
| spelling | doaj.art-117d498d16cb40f8bce3afa9019de83e2022-12-22T02:32:42ZengWiley-VCHChemistryOpen2191-13632022-06-01116n/an/a10.1002/open.202200039Strained Ammonium Precursors for RadiofluorinationsDr. Falco Reissig0Dr. Constantin Mamat1Institut für Radiopharmazeutische Krebsforschung Helmholtz-Zentrum Dresden-Rossendorf Bautzner Landstraße 400 01328 Dresden GermanyInstitut für Radiopharmazeutische Krebsforschung Helmholtz-Zentrum Dresden-Rossendorf Bautzner Landstraße 400 01328 Dresden GermanyAbstract The increasing application of positron emission tomography (PET) in nuclear medicine has stimulated the extensive development of a multitude of novel and versatile techniques to introduce fluorine‐18, especially for the radiolabelling of biologically or pharmacologically active molecules. Taking into consideration that the introduction of fluorine‐18 (t1/2=109.8 min) mostly proceeds under harsh conditions, radiolabelling of such molecules represents a challenge and is of enormous interest. Ideally, it should proceed in a regioselective manner under mild physiological conditions, in an acceptable time span, with high yields and high specific activities. Special attention has been drawn to 2‐fluoroethyl and 3‐fluoropropyl groups, which are often the active sites of radiofluorinated compounds. Precursors containing an ammonium leaving group – such as a strained azetidinium or aziridinium moiety – can help to overcome these obstacles leading to a convenient and mild introduction of [18F]fluoride with high radiochemical yields.https://doi.org/10.1002/open.202200039azetidiniumaziridinesfluorinationring openingstrained rings |
| spellingShingle | Dr. Falco Reissig Dr. Constantin Mamat Strained Ammonium Precursors for Radiofluorinations ChemistryOpen azetidinium aziridines fluorination ring opening strained rings |
| title | Strained Ammonium Precursors for Radiofluorinations |
| title_full | Strained Ammonium Precursors for Radiofluorinations |
| title_fullStr | Strained Ammonium Precursors for Radiofluorinations |
| title_full_unstemmed | Strained Ammonium Precursors for Radiofluorinations |
| title_short | Strained Ammonium Precursors for Radiofluorinations |
| title_sort | strained ammonium precursors for radiofluorinations |
| topic | azetidinium aziridines fluorination ring opening strained rings |
| url | https://doi.org/10.1002/open.202200039 |
| work_keys_str_mv | AT drfalcoreissig strainedammoniumprecursorsforradiofluorinations AT drconstantinmamat strainedammoniumprecursorsforradiofluorinations |