Suppr超能文献

合成苯并噻唑的绿色方法学发展的最新进展

Recent Advances in the Development of Greener Methodologies for the Synthesis of Benzothiazoles.

作者信息

Saha Nirjhar, Kumar Asim, Debnath Bibhuti Bhusan, Sarkar Anirban, Chakraborti Asit K

机构信息

School of Chemical Sciences, Indian Association for the Cultivation of Science (IACS), Jadavpur, Kolkata, West Bengal 700 032, India.

Amity Institute of Pharmacy, Amity University Haryana, Manesar, India-122413.

出版信息

Curr Top Med Chem. 2025;25(5):581-644. doi: 10.2174/0115680266347975241217112119.

Abstract

The benzothiazole ring system has been recognised with crucial pharmacophoric features being present among various approved drugs and clinical and pre-clinical candidates. The medicinal importance of this privileged scaffold stimulated the interest of synthetic medicinal/ organic chemists for the synthesis of its derivatives due to their diverse biological applications. In most of the reports in the literature, benzothiazoles were synthesized by cyclocondensation of 2- aminothiophenol with either carboxylic acid and its derivatives or aldehydes. However, many of these procedures involve reaction conditions that are not in conformity with sustainable chemistry development. The negative impact of chemicals and their manufacturing processes on the environment, human health, and biodiversity raises safety concerns. On the other hand, the utilization of non-renewable energy sources, use of rare earth metals as catalysts, involvement of costly chemicals, prolonged reaction time at high temperatures, and considerable waste generation diminish the greener impact of these reaction methodologies and make them non-sustainable. In order to avoid such drawbacks of the non-sustainable practices in the synthesis of benzothiazoles, there have been continuous efforts to develop greener methodologies for the construction of this bioactive scaffold. This review aims to delve into the literature reports on the recent advancements in the development of greener methodologies for the synthesis of bioactive benzothiazoles.

摘要

苯并噻唑环系在各种已批准药物以及临床和临床前候选药物中具有关键的药效基团特征,这一点已得到认可。由于其多样的生物学应用,这种具有特殊地位的骨架的药用重要性激发了合成药物/有机化学家对其衍生物合成的兴趣。在文献中的大多数报道中,苯并噻唑是通过2-氨基硫酚与羧酸及其衍生物或醛的环缩合反应合成的。然而,这些方法中的许多都涉及不符合可持续化学发展的反应条件。化学品及其制造过程对环境、人类健康和生物多样性的负面影响引发了安全担忧。另一方面,不可再生能源的利用、使用稀土金属作为催化剂、使用昂贵的化学品、高温下延长的反应时间以及大量废物的产生,削弱了这些反应方法的绿色影响,使其不可持续。为了避免苯并噻唑合成中不可持续做法的此类缺点,人们一直在不断努力开发更绿色的方法来构建这种生物活性骨架。本综述旨在深入探讨有关合成生物活性苯并噻唑的更绿色方法开发的最新进展的文献报道。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验