A novel and efficient one-pot synthesis of symmetrical diamide (bis-amidate) prodrugs of acyclic nucleoside phosphonates and evaluation of their biological activities.

@article{Jansa2011ANA,
  title={A novel and efficient one-pot synthesis of symmetrical diamide (bis-amidate) prodrugs of acyclic nucleoside phosphonates and evaluation of their biological activities.},
  author={Petr Jansa and Ondřej Baszczyňski and Martin Dra{\vc}{\'i}nsk{\'y} and Ivan Votruba and Zdeněk Z{\'i}dek and Gina Bahador and George Stepan and Tom{\'a}{\vs} Cihl{\'a}ř and Richard L Mackman and Anton{\'i}n Hol{\'y} and Zlatko Janeba},
  journal={European journal of medicinal chemistry},
  year={2011},
  volume={46 9},
  pages={3748-54}
}
A novel and efficient method for the one-pot synthesis of diamide (bis-amidate) prodrugs of acyclic nucleoside phosphonates, starting from free phosphonic acids or phosphonate diesters is reported. The approach from phosphonate diesters via their bis(trimethylsilyl) esters is highly convenient, eliminates isolation and tedious purification of the phosphonic acids, and affords the corresponding bis-amidates in excellent yields (83-98%) and purity. The methodology has been applied to the… CONTINUE READING

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