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Merck

Solvent-free synthesis of pyrimidine nucleoside-aminophosphonate hybrids and their biological activity evaluation.

Nucleosides, nucleotides & nucleic acids (2010-07-28)
Xinying Zhang, Yingying Qu, Xuesen Fan, C Bores, Dong Feng, Graciela Andrei, Robert Snoeck, Erik De Clercq, Philippe M Loiseau
ABSTRAKT

A novel and highly efficient one-pot three-component synthesis of alpha-aminophosphonates under neat condition was developed. By employing this method, hybrid compounds of aminophosphonate with pyrimidine nucleosides were synthesized in good to excellent yields starting from 5-formyl-2'-deoxyuridine, aniline and dimethyl phosphite. The antiviral and antileishmanial activities of these novel hybrid compounds were also studied but none were found to be active.

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Sigma-Aldrich
Dimethyl phosphite, 98%