Process research on the preparation of DMT protected 2'-O-methoxyethylguanosine for oligonucleotide synthesis in therapeutic applications.

摘要

An optimized process to synthesize DMT protected 2 '-O-methoxyethylguanosine is described. A key step involves the enzymatic deamination of a mixture of alkylated products to selectively afford the desired material without resorting to chromatography for purification. This approach was scaled up to kilogram quantities for use in oligonucleotide therapeutics. [formula: see text].