摘要 |
The invention relates to the chemical synthesis of oligonucleotides and to chemical entities useful in such synthesis. More particularly, the invention relates to sulfurization of the internucleoside linkages of oligonucleotides. The invention provides new sulfur transfer reagents of formula (1) and processes for their use in sulfurizing oligonucleotides. The sulfur transfer reagents according to the invention are inexpensive to make, stable in storage, and highly efficient in sulfurization. In Formula (1) n = 1 to 4, and wherein R can be the same as or different from R<1>, and wherein R and R<1> are selected from the group consisting of CH3, CH2CH3, tert-butyl, Formula (2), (3), (4), wherein R<2>, R<3> and R<4>, are selected from the group consisting of Cl, Br, I, CN, NO2, CH3, and CH2CH3, and wherein R<1>, R<2>, R<3> and R<4>, taken separately are hydrogen, lower alkyl, electron-withdrawing substituted lower alkyl, lower alkyl- or halo-substituted aryl, or a heterocycle containing nitrogen, oxygen, or sulfur and from 5-8 carbon atoms. |