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- W182578986 abstract "This chapter describes two general methods for attaching conjugate groups to oligonucleotides containing alkylamine linker arms. It uses a simple acylation reaction with a variety of activated esters for the preparation of hundreds of oligonucleotide conjugates. The first method (Method A) describes reaction of high-performance liquid chromatography (HPLC)-purified amine-modified oligonucleotides under anhydrous conditions. Triethylammonium (TEA) salts of oligonucleotides are soluble in dimethyl sulfoxide (DMSO) and allow the successful conjugation of lipophilic and hydrolytically unstable groups in homogeneous organic solution. The anhydrous conditions also protect the electrophile from hydrolysis and require only a small excess of conjugate group. This versatile method has been used to prepare all three major types of oligonucleotide conjugates. The second method (Method B) describes acylation of 5'–alkylamine-modifled ofigonucleotides while still immobilized on the solid support. This simpler method has advantages for conjugate groups that can survive oligonucleotide deprotection conditions. The two general methods are compared by preparing a specific oligonucleotide conjugate: an oligodeoxynucleotide (ODN) with a 5'-minor groove-binding (MGB) conjugate group." @default.
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- W182578986 date "2000-01-01" @default.
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- W182578986 title "Synthesis of oligonucleotide conjugates in anhydrous dimethyl sulfoxide" @default.
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- W182578986 doi "https://doi.org/10.1016/s0076-6879(00)13011-3" @default.
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