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Some Features of the Tscherniac‒Einhorn Reaction with 2-Thiouracil Derivatives
Russian Journal of General Chemistry ( IF 0.9 ) Pub Date : 2020-06-04 , DOI: 10.1134/s1070363220030056
I. A. Novakov , D. S. Sheikin , V. V. Chapurkin , M. B. Navrotskii , A. S. Babushkin , E. A. Ruchko , A. Yu. Maryshev , D. Schols

Abstract

The Tscherniac–Einhorn reaction of 6-methyl and 6-(trifluoromethyl) derivatives of 2-thiouracil with N-(bromomethyl)phthalimide in under basic catalysis leads to the formation of S-amidomethylation products. When using 6-amino-2-thiouracil, decomposition of the alkylation products occurs. An in vitro study of the compounds obtained showed their lack of cytotoxicity and anti-HIV-1/2 activity.


中文翻译:

Tscherniac‒Einhorn与2-硫脲嘧啶衍生物的反应的一些特征

摘要

在碱性催化下2-硫尿嘧啶的6-甲基和6-(三氟甲基)衍生物与N-(溴甲基)邻苯二甲酰亚胺的Tscherniac-Einhorn反应导致形成S-酰胺甲基化产物。当使用6-氨基-2-硫尿嘧啶时,发生烷基化产物的分解。对获得的化合物的体外研究表明,它们缺乏细胞毒性和抗HIV-1 / 2活性。
更新日期:2020-06-04
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