A PROSTHETIC GROUP FOR THE RAPID INTRODUCTION OF FLUORINE INTO PEPTIDES AND FUNCTIONALIZED DRUGS

一种用于将氟快速引入肽和功能化药物的假体基团

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Abstract

Fluoride ion as the tetrabutylammonium salt displaces bromide in para-substituted benzyl bromides in acetonitrile or dimethylformamide. The p-bromomethyl benzoyl (BMB) group has been coupled to amino groups, including peptide amino groups, via its N-hydroxysuccinimide ester. In a subsequent step, the facile displacement of bromide by fluoride occurred under conditions compatible for use with (18)F radiotracers.

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