| 摘要 |
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.lambda.6-benzo[d]isothiazol-3-one, preferably in the presence of a n organic base. The 1,1-dioxo-1,2-dihydro-1.lambda.6-benzo[d]isothiazol-3-one is represented by the following structural formula: (I); wherein p is 0 or an integer from 1 to 4; X7 is O or S; R for each occurence is a substituent, preferably each independently, a halo, a substituted or unsubstituted aliphatic group, -NR11R12, -OR13, -OC(O)R13, -C(O)OR13, 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; R11 and R12 are each, independently, -H, a substituted or unsubstituted aliphatic group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aralkyl group; and R13 is 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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