Process research on the preparation of DMT protected 2'-O-methoxyethylguanosine for oligonucleotide synthesis in therapeutic applications.
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].
Taj
Shabbir Ali S
SA
Isis Pharmaceuticals, Inc., Carlsbad, California, USA.
Narayanan
S
S
Meenakshi
S Suman
SS
Sanghvi
Yogesh S
YS
Ross
Bruce S
BS
Ravikumar
Vasulinga T
VT
D000243:Adenosine Deaminase / Q000737:chemistry; D002851:Chromatography, High Pressure Liquid; D005786:Gene Expression Regulation / Q000235:genetics*; D006151:Guanosine / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D013058:Mass Spectrometry; D015394:Molecular Structure; D009841:Oligonucleotides / Q000138:chemical synthesis* / Q000235:genetics
C484916:2'-O-methoxyethylguanosine; D009841:Oligonucleotides; D006151:Guanosine; D000243:Adenosine Deaminase