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一种通过使用“可挥发”载体合成3,4-二取代-2-氨基噻唑鎓衍生物的简便方法。

A Facile Approach to the Synthesis of 3,4-Disubstituted-2-Aminothiazolium Derivatives through the Use of A "Volatilizable" Support.

作者信息

Li Yangmei, Giulianotti Marc, Houghten Richard A

机构信息

Torrey Pines Institute for Molecular Studies, 11350 Village Parkway, Port St. Lucie, FL 34987.

出版信息

Tetrahedron Lett. 2010 Oct 27;51(43):5637-5639. doi: 10.1016/j.tetlet.2010.08.026.

DOI:10.1016/j.tetlet.2010.08.026
PMID:21765557
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3133972/
Abstract

A facile solid-phase synthetic approach to the synthesis of 3,4-disubstituted-2-aminothiazolium derivatives was reported. Functionalized aminomethylphenyl silica gel was used as a "volatilizable" support. The products were cleaved with 10% HF and were obtained in high yields and purities.

摘要

报道了一种简便的固相合成方法用于合成3,4-二取代-2-氨基噻唑鎓衍生物。功能化的氨甲基苯基硅胶被用作“可挥发”载体。产物用10%的氢氟酸裂解，以高收率和高纯度得到。

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本文引用的文献

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High throughput synthesis of peptide alpha-thioesters through the use of "volatilizable" support.通过使用“可挥发”载体进行肽α-硫酯的高通量合成。
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Activity of rat cytosolic thioredoxin reductase is strongly decreased by trans-[bis(2-amino-5- methylthiazole)tetrachlororuthenate(III)]: first report of relevant thioredoxin reductase inhibition for a ruthenium compound.
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Synthesis and biological evaluation of analogues of the anti-tumor alkaloid naamidine A.抗肿瘤生物碱那米定A类似物的合成及生物学评价
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2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor.2-氨基噻唑作为一种新型激酶抑制剂模板。关于发现N-(2-氯-6-甲基苯基)-2-[[6-[4-(2-羟乙基)-1-哌嗪基)]-2-甲基-4-嘧啶基]氨基]-1,3-噻唑-5-甲酰胺（达沙替尼，BMS-354825）作为一种强效泛Src激酶抑制剂的构效关系研究。
J Med Chem. 2006 Nov 16;49(23):6819-32. doi: 10.1021/jm060727j.
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Bioorg Med Chem Lett. 2006 May 15;16(10):2800-3. doi: 10.1016/j.bmcl.2006.01.126. Epub 2006 Feb 23.
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