Vinyl substituted radiohalogen conjugates for protein labeling

Details Vinyl substituted radiohalogen conjugates for protein labeling Vinyl substituted radiohalogen conjugates for protein labeling

1989-07-05

1993-04-06

Stoll, Robert L.

Drug, bio-affecting and body treating compositions

Radionuclide or intended radionuclide containing; adjuvant...

5303915, 530402, 514 2, 560104, 570182, C07D20746, C07C 6976, C07C 6962, A61K 6902

Patent

active

052001695

ABSTRACT:
Vinyl radiohalogenated small molecules as shown in formulas I and II: ##STR1## wherein *X is radiohalogen, C.dbd.C is a double bonded set of sp.sup.2 hybridized carbon atoms, and substituents R.sub.1, and R.sub.2 are as defined in the specification. Y is a substituent containing any of the groups described for R.sub.1 and R.sub.2, except that Y cannot be hydrogen, and bearing a functional group suitable for binding to protein under conditions that preserve the biological activity of the protein. The compounds of formulas I and II can be coupled to proteins such as monoclonal antibodies to provide reagents for diagnostic and therapeutic applications. Also metalated precursors of compounds I and II, as well as radiopharmaceutical reagent kits containing any of the subject small molecules.

REFERENCES:
patent: 4450149 (1984-05-01), Kabalka
patent: 4524059 (1985-06-01), Elmaleh et al.
patent: 4541957 (1985-09-01), Nakatsuka et al.
patent: 4725426 (1988-02-01), Hofmeister et al.
patent: 4755323 (1988-07-01), Eidenschink et al.
patent: 4870188 (1989-09-01), Wilbur et al.
Kabalka et al., J. Lab Cmpds. & Radiopharm., "Synthesis of I-125 Labeled Aryl and Vinyl Iodides", vol. 19, No. 6, 1982, pp. 795-799.
Hanson, R. N. et al., E-17.alpha.-[.sup.125 I]iodovinylestradiol: an estrogen-receptor-seeking radiopharmaceutical, J. Nucl. Med. 23(5):431-436, 1982.
Hanson, R. N. et al., Radiohalodestannylation: Synthesis of .sup.125 I-Labeled 17.alpha.-E-iodovinylestradiol, Int. J. Appl. Radiat. Isot. 35(8): 810-812, 1984.
Hoyte, R. M. et al., Synthesis and Evaluation of Potential Radioligands for the Progesterone Receptor, J. Med. Chem. 28(11):1695-1699, 1985.
March, J., Advanced Organic Chemistry, Third Edition, John Wiley & Sons, pp. 664-666, 1985.
Goodman, M. M. et al., Design, Synthesis and Evaluation of 2-deoxy-2-iodovinyl-branched Carbohydrates as Potential Brain Imaging Agents, Proceedings of the Sixth International Symposium on Radiopharmaceutical Chemistry, Boston, Ma., Jun. 29-Jul. 3, 1986, in Journal of Labelled Compounds and Radiopharmaceuticals 23:243-245, 1987.
Salisbury, L. E., Kinetic Study of the Relationship of Rearrangement to Racemization in Certain Dibenzo [a,e]cyclooctatetraenes, J. Org. Chem. 43(26):4991-4995, 1978.
Schwartz, J. and J. A. Labinger, Hydrozirconation: A New Transition Metal Reagent for Organic Synthesis, Agnew Chem. Int. Ed. Engl. 15(6):333-340, 1976.
Seyferth, D., "Vinyl Derivatives of the Metals. III. Vinylmercuric halides," The Journal of Organic Chemistry 22:478, 1957.
Larock, R. C. et al., Reaction of 2-alkenyl-1,3,2-benzodioxaboroles with Mercuric Acetate: a Convenient Stereospecific Procedure for the Conversion of Alkynes into Alkenylmercuric Salts, J. Amer. Schem. Soc. 94(12):4371-4373, 1982.
Kabalka, G. W., et al., Rapid and Mild Syntheses of Radioiodinated Estrogen Derivatives via Organoborane Technology, in Applications of Nuclear and Radiochemistry, M. Lambrecth and N. Morcos, Eds., Brookhaven National Laboratory, Pergamon Press, pp. 197-203, 1982.
Kabalka, G. W., et al., A Convenient Procedure for the Synthesis of Vinyl Iodides via the Reaction of Iodine Monochloride with Vinylboronic Acids, Synthetic Communications 11(3):247-251, 1981.
Chemical Abstracts, 97(25):788, ABstract No. 215434, Dec. 20, 1982.
Adam, M. J., "The Demetallation Reaction in Radiohalogen Labelling: Synthesis of Bromine and Fluorine Labelled Components," Int. J. Radiat. Appl. Instrum. Part A, Appl. Radiat. Isotl 37(8):811-815, 1986.

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