Synthesis of oligonucleotides or phosphorothioate...

Details Synthesis of oligonucleotides or phosphorothioate... Synthesis of oligonucleotides or phosphorothioate...

2008-10-10

2011-10-18

Crane, Lawrence E (Department: 1623)

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

Reexamination Certificate

active

08039612

ABSTRACT:
According to the present invention, there is provided a process for making an oligonucleotide or a phosphorothioate oligonucleotide. The process has the following steps: (a) providing an amount of a blocked nucleotide; (b) deblocking the blocked nucleotide to form an unblocked nucleotide; (c) activating the deblocked nucleotide; (d) coupling the deblocked nucleotide with a phosphoramidite to form a phosphite oligomer; (e) capping any uncoupled deblocked nucleotide via reaction with an amount of acetic anhydride and an amount of N-methylimidazole that is substantially free of 1,3,5-trimethylhexahydro-1,3,5-triazine; (f) oxidizing the phosphite oligomer to form the oligonucleotide or sulfurizing the phosphite oligomer to form a phosphorothioate oligonucleotide; and (g) optionally repeating steps (b) through (f). There is also a process for capping a nucleotide.

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Sobczyk et al.; “Infrared and NMR Spectroscopic Studies of Hexhydro-1,3,5-Trialkyltriazines”; Chemia Stosowana (1973) 17 (3); pp. 359-366.

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