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吡唑啉衍生物的各种合成方法及合成参数的比较。

Comparison of various synthesis methods and synthesis parameters of pyrazoline derivates.

作者信息

Praceka Meilinda Setya, Megantara Sandra, Maharani Rani, Muchtaridi Muchtaridi

机构信息

Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran, 45363, Jatinangor, West Java, Indonesia.

Department of Chemistry, Faculty of Mathematics and Natural Science, Universitas Padjadjaran, Sumedang, West Java, Indonesia.

出版信息

J Adv Pharm Technol Res. 2021 Oct-Dec;12(4):321-326. doi: 10.4103/japtr.JAPTR_252_21. Epub 2021 Oct 20.

DOI:10.4103/japtr.JAPTR_252_21
PMID:34820304
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8588918/
Abstract

Pyrazoline plays an important role in the development of heterocyclic chemistry theory and is widely used as a synthesis useful in organic synthesis. The structure of the pyrazoline derivative compound contains a 5-membered heterocyclic framework with two nitrogen atoms and one endocyclic double bond. The function of pyrazoline as a fragment was stable enough in the bioactive group to synthesize new compounds with various biological activities. Various methods that could be used for the synthesis of pyrazole derivatives were ultrasonic irradiation, microwave assistance, ionic liquids, grinding techniques, and conventional methods. However, the synthesis of pyrazoline derivatives using conventional methods had many problems, one of which is the product yield, which was <70%. Therefore, this article will discuss the importance of optimizing the synthesis reaction conditions by taking into account several synthesis parameters to get the best organic product results based on conventional methods. A literature search was conducted by employing PubChem, Chemspider Google Scholar, Research Gate, Science Direct, and Elsevier by selecting pyrazoline synthesis based on physicochemical profile, reaction mechanism, and synthesis method.

摘要

吡唑啉在杂环化学理论的发展中起着重要作用,并且在有机合成中作为一种有用的合成试剂被广泛应用。吡唑啉衍生物化合物的结构包含一个具有两个氮原子和一个环内双键的五元杂环骨架。吡唑啉作为片段在生物活性基团中足够稳定,可用于合成具有各种生物活性的新化合物。可用于合成吡唑啉衍生物的各种方法有超声辐射、微波辅助、离子液体、研磨技术和传统方法。然而,使用传统方法合成吡唑啉衍生物存在许多问题,其中之一是产物产率,其低于70%。因此,本文将讨论基于传统方法考虑几个合成参数来优化合成反应条件以获得最佳有机产物结果的重要性。通过使用PubChem、Chemspider、谷歌学术、Research Gate、Science Direct和Elsevier进行文献检索,选择基于物理化学性质、反应机理和合成方法的吡唑啉合成。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d3f/8588918/3b3aa17891a5/JAPTR-12-321-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d3f/8588918/673f1f3f1359/JAPTR-12-321-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d3f/8588918/654ac7cec8a4/JAPTR-12-321-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d3f/8588918/432a7e5b0061/JAPTR-12-321-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d3f/8588918/6fd5ed4de734/JAPTR-12-321-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d3f/8588918/3b3aa17891a5/JAPTR-12-321-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d3f/8588918/673f1f3f1359/JAPTR-12-321-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d3f/8588918/654ac7cec8a4/JAPTR-12-321-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d3f/8588918/432a7e5b0061/JAPTR-12-321-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d3f/8588918/6fd5ed4de734/JAPTR-12-321-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d3f/8588918/3b3aa17891a5/JAPTR-12-321-g005.jpg

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Antitumor activity of novel pyrazole-based small molecular inhibitors of the STAT3 pathway in patient derived high grade glioma cells.新型基于吡唑的 STAT3 通路小分子抑制剂在患者来源的高级别神经胶质瘤细胞中的抗肿瘤活性。
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Design and Synthesis of Pyrazole-3-one Derivatives as Hypoglycaemic Agents.作为降血糖剂的吡唑 - 3 - 酮衍生物的设计与合成
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