Process for introducing fluorine into biologically active materi

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Insulin; related peptides

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530345, 424 11, 536 26, 544271, 544276, 560 41, 562438, 564184, 564185, C07K 102, C07K 740, C07D47306, C07H 19168

Patent

active

050989960

ABSTRACT:
Radioactive fluorine can be easily introduced into biologically active molecules containing amino groups. A p-bromomethyl benzoyl group is coupled to the amino group of the biologically active molecule, and bromine is displaced by fluorine. Alternatively, the bromine on the bromomethylbenzoyl group is first displaced by fluorine, and the fluoromethyl benzoyl group is then coupled to the amino group of the biologically active molecule. The compounds so produced are useful in diagnostic nuclear medicine.

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patent: 4617386 (1986-10-01), Elmaleh et al.
patent: 4647446 (1987-03-01), Sargent, III et al.
patent: 4647447 (1987-03-01), Gries et al.
Morrison and Boyd, Organic Chemistry, 3rd edition, (Boston, Allen and Bacon, 1979), pp. 1148 to 1149.
Fieser and Fieser, Reagents for Organic Synthesis [New York, John Wiley and Sons, 1967], pp. 485 to 487.

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