ORGN 420 |
Synthesis of a bifunctional PEG-linker for the attachment of amines to oligonucleotides
| Kim B. Jensen1, Søren N. Jakobsen1, and Jakob Felding2. (1) Nuevolution A/S, Rønnegade 8, DK-2100 Copenhagen, Denmark, (2) BioImage A/S, Mørkhøj Bygade 28, DK-2960 Søborg, Denmark |
| A solid phase method to prepare polyethylene glycol linked amino compounds 4 has been developed to support our Chemetics® technology. The key steps of the method were the synthesis of a hetero bifunctional polyethylene glycol linker attached to a 2-chlorotrityl resin (2) and subsequent derivatization of 2 by using a Mitsunobu protocol. For the validation of the polyethylene glycol linked protocol the compound 5 and the conjugated oligonucleotide 6 were synthesised. The ability of 5 to bind to the αvβ3 integrin receptor was investigated in a competition ELISA experiment and compared to known ligands and the conjugated oligonucleotide 6 was used in a selection experiment with an immobilized αvβ3 integrin receptor. 
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Total Synthesis, Process R&D, Combinatorial, Bioorganic, Physical Organic Chemistry
8:00 PM-10:00 PM, Tuesday, August 24, 2004 Pennsylvania Convention Center -- Hall D, Poster
Sci-Mix
8:00 PM-10:00 PM, Monday, August 23, 2004 Pennsylvania Convention Center -- Hall D, Sci-Mix
Division of Organic Chemistry
The 228th ACS National Meeting, in Philadelphia, PA, August 22-26, 2004
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