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Efficient large-scale synthesis of 5'-O-dimethoxytrityl-N4-benzoyl-5-methyl-2'-deoxycytidine
Bruce S Ross1, Mingming Han, Vasulinga T Ravikumar
1Isis Pharmaceuticals, Inc., 2282 Faraday Ave., Carlsbad, CA 92008, USA.
Abstract:
An efficient process to synthesize 5'-O-dimethoxytrityl-N4-benzoyl-5-methyl-2'-deoxycytidine in high yield and quality is described. Final benzoylation was improved by developing a method to selectively hydrolyze benzoyl ester impurities. This inexpensive approach was scaled up to multikilogram quantities for routine use in oligonucleotide therapeutics.
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