Radiosynthesis of [18F]-Labelled Pro-Nucleotides (ProTides)
نویسندگان
چکیده
منابع مشابه
18F-Labelled Intermediates for Radiosynthesis by Modular Build-Up Reactions: Newer Developments
This brief review gives an overview of newer developments in (18)F-chemistry with the focus on small (18)F-labelled molecules as intermediates for modular build-up syntheses. The short half-life (<2 h) of the radionuclide requires efficient syntheses of these intermediates considering that multistep syntheses are often time consuming and characterized by a loss of yield in each reaction step. R...
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The present paper is concerned with radiochemical methodology to furnish the trifluoromethyl motif labelled with (18)F. Literature spanning the last four decades is comprehensively reviewed and radiochemical yields and specific activities are discussed.
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The masking of nucleoside phosphate and phosphonate groups by an aryl motif and an amino acid ester, nowadays known as the 'ProTide' technology, has proven to be effective in the discovery of nucleotide therapeutics. Indeed, this technology, which was invented by Chris McGuigan in the early 1990s, has inspired the discovery of two FDA-approved antiviral nucleotide drugs, and many more are curre...
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Nucleophilic 18F-fluorination of bromodifluoromethyl derivatives was performed using [18F]Bu4NF in the presence of DBU (1,8-diazabicyclo[5.4.0]undec-7-ene). This novel procedure provided a diverse set of [18F]trifluoroacetamides in good to excellent radiochemical conversions. A mechanism where DBU acts as organomediator in this transformation is proposed.
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ژورنال
عنوان ژورنال: Molecules
سال: 2020
ISSN: 1420-3049
DOI: 10.3390/molecules25030704