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

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
ABSTRACT

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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Dimethyl phosphite, 98%