Synthesis of phosphorofluoridates and phosphorofluoridothioates via the phosphoramidite approach |
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Authors: | Dabkowski Wojciech Tworowska Izabela |
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Institution: | Centre of Molecular and Macromolecular Studies, Polish Academy of Sciences, 90-363, ?ód?, Sienkiewicza 112, Poland. wdabkow@bilbo.cbmm.lodz.pl |
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Abstract: | We present a very efficient synthetic procedure leading to the phosphorofluoridates RO-P(O)(OH)F 1 or phosphorofluoridothioates RO-P(S)(OH)F 2, which is based on the intermediary of fluorophosphoramidites (RO)P(F)N(i)Pr2 5 R = 9-(hydroxyethyloxymethyl)guaninyl), 3'azido-3'deoxythymidinyl, thymidinyl, anhydrothymidinyl, cholesteryl, N6-benzoyl-5'-O-(4,4'-dimethoxytrityl)-2'-deoxyadenosinyl]. The activation of the amino group was performed with trimethylchlorosilane (TMCS). |
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