Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives
Patent
1995-05-22
1997-05-20
Kunz, Gary L.
Organic compounds -- part of the class 532-570 series
Organic compounds
Carbohydrates or derivatives
536 253, C07H 102, C07H 2100
Patent
active
056313616
ABSTRACT:
The present invention comprises a novel method of incorporating radiolabels and other type of labels at one or more predetermined sites within an oligonucleotide. In particular, the method comprises contacting a nascent, support-bound oligonucleotide having an unprotected 5' hydroxyl group with a suitable activating agent, followed by contacting the resulting activated nascent oligonucleotide with a labeled, Y-protected mononucleotide having an unprotected 3'-hydroxyl, thereby condensing the labeled mononucleotide and nascent oligonucleotide. Normal automated synthesis can then be continued to yield the oligonucleotide of desired length having the label in the desired location. This method advantageously yields oligonucleotides with high specific activity. The oligonucleotides thereby produced are useful for determining the pharmacokinetics and biodistribution of their non-radiolabeled counterparts, both in vitro and in vivo.
REFERENCES:
patent: 5047524 (1991-09-01), Andrus et al.
patent: 5281701 (1994-01-01), Vinayak et al.
Cao et al. Tetrahedron Lett. 24(10): 1019-1020, 1983.
Agrawal Sudhir
Iyer Radhakrishnan P.
Jiang Zhiwei
Tan Weitian
Yu Dong
Greenfield Michael S.
Hybridon, Inc.
Kunz Gary L.
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