Avecia Biotechnology, Inc.

William Edward Zedalis

Nanda Dulal Sinha

Gregory Keith Miranda

A process for the synthesis of oligonucleotides using phosphoramidite chemistry is provided. The process employs as activator a 1,1-dioxo-1,2-dihydro-1&#x3bb;-benzo[d]isothiazol-3-one, preferably in the presence of an organic base. The 1,1-dioxo-1,2-dihydro-1&#x3bb;-benzo[d]isothiazol-3-one is represented by the following structural formula: 

Activators for oligonucleotide synthesis

A process for the synthesis of oligonucleotides using phosphoramidite chemistry is provided. The process employs as activator a 1,1-dioxo-1,2-dihydro-1&#x3bb;-benzo[d]isothiazol-3-one, preferably in the presence of an organic base. The 1,1-dioxo-1,2-dihydro-1&#x3bb;-benzo[d]isothiazol-3-one is represented by the following structural formula: wherein p is 0 or an integer from 1 to 4; Xis O or S; R for each occurrence is a substituent, preferably each independently, a halo, a substituted or unsubstituted aliphatic group, &#x2014;NRR, &#x2014;OR, &#x2014;OC(O)R, &#x2014;C(O)OR, or cyano; or two adjacent R groups taken together with the carbon atoms to which they are attached form a six membered saturated or unsaturated ring; Rand Rare each, independently, &#x2014;H, a substituted or unsubstituted aliphatic group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aralkyl group; and Ris a substituted or unsubstituted aliphatic group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aralkyl group. Preferred organic bases are pyridine, 3-methylpyridine, or N-methylimidazole.

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Fitchburg, MA, United States of America

William Edward Zedalis