Organic compounds -- part of the class 532-570 series – Organic compounds – Unsubstituted hydrocarbyl chain between the ring and the -c-...
Patent
1993-12-30
1996-09-10
Datlow, Philip I.
Organic compounds -- part of the class 532-570 series
Organic compounds
Unsubstituted hydrocarbyl chain between the ring and the -c-...
540467, 540474, C07D25502, C07D25702, C07D27300
Patent
active
055547486
ABSTRACT:
There are provided polychelants and their metal chelates which are useful in diagnostic imaging and in radiotherapy and which comprise a plurality of macrocyclic chelant moieties, e.g. DOTA residues, conjugated to a polyamine backbone molecule, e.g. polylysine. To produce a site-specific polychelate, one or more of the macrocyclic chelant carrying backbone molecules may be conjugated to a site-directed macromolecule, e.g. a protein. For example, adducts of a macrocyclic chelant can be formed by the process of (a) dispersing a carboxylic macrocyclic chelant in a polar, anhydrous solvent, (b) adding a base with a pKa sufficient to remove all carboxyl protons to create an amine salt of the chelant soluble in the solvent, (c) chilling the reaction mixture to between about 5.degree. C. and 55.degree. C. above the freezing point of the solvent, and (d) adding substantial equimolar amount of chilled alkylhaloformate under anhydrous conditions so as to form a slurry containing the mixture carboxycarbonic anhydride of the chelant.
REFERENCES:
patent: 4647447 (1987-03-01), Gries et al.
patent: 4741900 (1988-05-01), Alvarez et al.
Krejcarek et al, Biochemical and Biophysical Research Comm, 77 (1977), pp. 581-585.
Sieving Paul F.
Watson Alan D.
Datlow Philip I.
Nycomed Salutar Inc.
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