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嘧啶核苷-氨基膦酸酯杂化物的无溶剂合成及其生物活性评价。

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

作者信息

Zhang Xinying, Qu Yingying, Fan Xuesen, Bores C, Feng Dong, Andrei Graciela, Snoeck Robert, De Clercq Erik, Loiseau Philippe M

机构信息

School of Chemistry and Environmental Sciences, Henan Key Laboratory for Environmental Pollution Control, Henan Normal University, Xinxiang, Henan, P. R. China.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2010 Aug;29(8):616-27. doi: 10.1080/15257770.2010.496281.

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.

摘要

开发了一种新颖且高效的在无溶剂条件下一锅法三组分合成α-氨基膦酸酯的方法。采用该方法,从5-甲酰基-2'-脱氧尿苷、苯胺和亚磷酸二甲酯出发,以良好至优异的产率合成了氨基膦酸酯与嘧啶核苷的杂化化合物。还研究了这些新型杂化化合物的抗病毒和抗利什曼原虫活性,但未发现有活性的化合物。

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