Nucleoside hydrogenphosphonates. Part 6. Reaction of nucleoside hydrogenphosphonates with arenesulphonyl chlorides

Abstract
The reaction of nucleoside 3′-hydrogenphosphonates (1) with 2,4,6-tri-isopropylbenzenesulphonyl chloride (TPS-Cl) in pyridine has been studied using 31P n.m.r. spectroscopy, and a general scheme for transformations occurring during this activation process is proposed. It was found that the reaction proceeded through several intermediates affording, as final products, the pyridine adduct of nucleoside 3′-metaphosphate (7), P1P2-bis-(S-aryl nucleosid-3′-yl) pyrophosphate (11a), and nucleoside S-aryl 3′-phosphorochloridate (13a), which upon addition of water were converted into nucleoside 3′-phosphate (2), P1P2-bis-(nucleosid-3′-yl) pyrophosphate (3), and nucleoside S-aryl 3′-phosphorothioate (4a).

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