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

Autor: Jacobson KA; Laboratory of Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, NIH, Bethesda, MD 20892 (U.S.A.)., Furlano DC; Laboratory of Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, NIH, Bethesda, MD 20892 (U.S.A.)., Kirk KL; Laboratory of Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, NIH, Bethesda, MD 20892 (U.S.A.).
Jazyk: angličtina
Zdroj: Journal of fluorine chemistry [J Fluor Chem] 1988 Jun; Vol. 39 (3), pp. 339-47. Date of Electronic Publication: 2001 Mar 01.
DOI: 10.1016/S0022-1139(00)81606-1
Abstrakt: 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.
Databáze: MEDLINE