We describe a new demethylation method for dimethyl phosphonate esters using sodium ethanethiolate. The new procedure allows demethylation of nucleoside dimethyl phosphonate esters without 1'-α-anomerization, providing an improved synthesis of 5'-methylene substituted 2',5'-deoxynucleotides.
Nan-Sheng Li, Joseph A Piccirilli, Geoffrey L Greene. Demethylation of dimethyl phosphonate esters with sodium ethanethiolate: Improved synthesis of 5'-methylene substituted 2',5'-deoxyribonucleotides. Nucleosides, nucleotides & nucleic acids. 2023;42(7):538-546
PMID: 36629008
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