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从苯乙酮卤化物中直接合成噻唑啉取代查耳酮。

Straightforward synthesis of thiazoline-incorporated chalconoids from phenacyl halides.

机构信息

Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Mazandaran University of Medical Sciences, Sari, Iran.

出版信息

Mol Divers. 2013 Feb;17(1):41-7. doi: 10.1007/s11030-012-9416-8. Epub 2013 Jan 12.

Abstract

A series of thiazoline-incorporated chalconoids, designed based on natural product scaffold, were efficiently synthesized via the reaction of 3-methyl-4-arylthiazole-2(3H)-thiones and appropriate phenacyl halides, and subsequent desulfurization. The starting 3-methyl-4- arylthiazole-2(3H)-thiones were also prepared from phenacyl halides. The structural aspects and (Z)-geometry of compounds were confirmed by IR and (1)H NMR spectral data. This chemistry provides a new library of compounds basically originated from phenacyl halides as building blocks, with potential activity for biomedical screening.

摘要

一系列基于天然产物骨架设计的噻唑啉取代查耳酮类化合物,通过 3-甲基-4-芳基-2(3H)-噻唑-2-硫酮与适当的苯乙酮卤化物反应,然后脱硫,高效合成。起始的 3-甲基-4-芳基-2(3H)-噻唑-2-硫酮也可以从苯乙酮卤化物制备得到。化合物的结构方面和(Z)-几何构型通过红外光谱(IR)和(1)H 核磁共振光谱(NMR)数据得到确认。这种化学方法提供了一个基本上由苯乙酮卤化物作为构建块衍生而来的新化合物库,具有用于生物医学筛选的潜在活性。

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