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通过Biginelli反应定向合成4H-嘧啶并[2,1-b]苯并噻唑衍生物的研究进展综述

Diversity Oriented Synthesis of 4H-Pyrimido[2,1-b]benzothiazole Derivatives via Biginellis Reaction: A Review.

作者信息

Gandhi Divyani, Kalal Priyanka, Prajapat Prakash, Agarwal Dinesh Kumar, Agarwal Shikha

机构信息

Department of Chemistry, Synthetic Organic Chemistry Laboratory, Mohanlal Sukhadia University, Udaipur, 313001 Rajasthan, India.

Department of Pharmocology, PAHER University, Udaipur, 313001 Rajasthan, India.

出版信息

Comb Chem High Throughput Screen. 2018;21(4):236-253. doi: 10.2174/1386207321666180330170456.

Abstract

BACKGROUND

Heterocycles have extended into widespread use for generating large collection of molecules in multi-component reactions. The development of new strategies for fused pyrimidobenzothiazole system has remained a highly attractive but challenging proposition for scientists working all around.

OBJECTIVE

The main objective of this work is to explore the utility of different catalysts as an ecofriendly reaction medium for green Biginellis reaction.

METHOD

A detailed study of Biginellis reactions using various catalysts was done using different research tools. The methods involved reaction of equimolar mixture of benzothiazole, 1,3-diketone and aldehyde as reactants by conventional and greener pathways via Knoevenagal condensation.

RESULTS

The present review has several significant advantages for the scientists regarding green synthesis viz. green conditions, short reaction times, high yields, clean reaction conditions, easy isolation of products, simple work-up procedure and mild reaction conditions.

CONCLUSION

Our report gives an overview of the combinatorial libraries for fused benzothiazole entities using metal catalyst, acid catalyst, ionic liquids, phase transfer catalyst, nano catalyst, etc.

摘要

背景

杂环化合物已广泛应用于多组分反应中以生成大量分子。对于世界各地的科学家而言,开发稠合嘧啶并苯并噻唑体系的新策略一直是一个极具吸引力但又充满挑战的课题。

目的

本研究的主要目的是探索不同催化剂作为绿色Biginelli反应的环境友好型反应介质的效用。

方法

使用不同的研究工具对使用各种催化剂的Biginelli反应进行了详细研究。这些方法涉及通过常规和更绿色的途径,经由Knoevenagel缩合反应,使苯并噻唑、1,3-二酮和醛的等摩尔混合物作为反应物进行反应。

结果

本综述在绿色合成方面为科学家提供了几个显著优势,即绿色条件、短反应时间、高收率、清洁的反应条件、产物易于分离、后处理程序简单以及反应条件温和。

结论

我们的报告概述了使用金属催化剂、酸催化剂、离子液体、相转移催化剂、纳米催化剂等构建稠合苯并噻唑实体的组合文库。

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