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首页> 外文期刊>Current Organocatalysis >Diversity Oriented p-TSA Catalyzed Efficient and Environmentally Benign Synthetic Protocol for the Synthesis of Structurally Diverse Heteroannulated Benzothiazolopyrimidines
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Diversity Oriented p-TSA Catalyzed Efficient and Environmentally Benign Synthetic Protocol for the Synthesis of Structurally Diverse Heteroannulated Benzothiazolopyrimidines

机译:面向多样性的p-TSA催化的高效,环境友好的合成方案,用于合成结构多样的杂环化苯并噻唑并嘧啶

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摘要

Diversity oriented synthetic protocol has been presented for the synthesis of structurally diverse drug -like small molecules. The present method involves three-component domino reaction of 2-aminobenzothiazoles, thiophene-2-carbaldehyde and carbonyl compounds in the presence of a catalytic amount of p-toluenesulphonic acid (p-TSA) as a recyclable and reusable eco-friendly acid catalyst in aqueous- alcoholic medium (C_2H_5OH- H_2O:v:v/ 1:5). The synthesis of structurally diverse heterocycles in very high yields (92-97%) from easily available starting materials, operational simplicity, mild reaction con-ditions, use of nontoxic and reusable acid catalyst, environmentally benign solvent system and shorter reaction time (10-48 min) at comparatively low temperature are special features of the present synthetic protocol.
机译:已经提出了面向多样性的合成方案,用于合成结构多样的药物样小分子。本方法涉及在催化量的对甲苯磺酸(p-TSA)的存在下,2-氨基苯并噻唑,噻吩-2-甲醛和羰基化合物的三组分多米诺反应,所述对甲苯磺酸是可回收和可重复使用的生态友好型酸催化剂。水性酒精介质(C_2H_5OH- H_2O:v:v / 1:5)。由易于获得的起始原料,高操作简便性,温和的反应条件,使用无毒且可重复使用的酸催化剂,对环境无害的溶剂体系和较短的反应时间以很高的收率(92-97%)合成结构多样的杂环在相对较低的温度下48分钟)是本合成规程的特殊功能。

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