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3-(2-氨基-1,6-二氢-6-氧代嘧啶-5-基)丙酸酯的多样性导向合成。

A diversity-oriented synthesis of 3-(2-amino-1,6-dihydro-6-oxo-pyrimidin-5-yl)propanoic esters.

机构信息

Grup d'Enginyeria Molecular, Institut Químic de Sarrià, Universitat Ramon Llull, Via Augusta 390, 08017, Barcelona, Spain.

出版信息

Mol Divers. 2011 May;15(2):595-601. doi: 10.1007/s11030-010-9287-9. Epub 2010 Nov 12.

DOI:10.1007/s11030-010-9287-9
PMID:21072589
Abstract

The synthesis of dimethyl 2-(methoxymethylene) pentanedioates by an unusual Michael addition of 3,3-dimethoxypropionate to α, β-unsaturated esters is described. These new intermediates can subsequently be converted to methyl 3-(2-amino-1,6-dihydro-6-oxo-pyrimidin-5-yl)propanoates upon treatment with guanidine carbonate. The resulting pyrimidine derivatives are open-chain analogues of pyrido[2,3-d]pyrimidines with interesting biological activities.

摘要

描述了 3,3-二甲氧基丙酸盐通过异常的迈克尔加成反应与α,β-不饱和酯加成合成二甲基 2-(甲叉基)戊二酸二甲酯。这些新的中间体随后可以与碳酸胍反应转化为甲基 3-(2-氨基-1,6-二氢-6-氧代嘧啶-5-基)丙酸盐。得到的嘧啶衍生物是具有有趣生物活性的吡啶并[2,3-d]嘧啶的开链类似物。

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本文引用的文献

1
An unusual Michael addition of 3,3-dimethoxypropanenitrile to 2-aryl acrylates: a convenient route to 4-unsubstituted 5,6-dihydropyrido[2,3-d]pyrimidines.3,3-二甲氧基丙腈与 2-芳基丙烯酸酯的非常规迈克尔加成反应：合成 4-未取代的 5,6-二氢吡啶并[2,3-d]嘧啶的便捷途径。
J Org Chem. 2010 Jan 15;75(2):487-90. doi: 10.1021/jo902345r.
2
Palladium-catalyzed cross-coupling of alpha-diazocarbonyl compounds with arylboronic acids.钯催化α-重氮羰基化合物与芳基硼酸的交叉偶联反应。
J Am Chem Soc. 2008 Feb 6;130(5):1566-7. doi: 10.1021/ja0782293. Epub 2008 Jan 11.
3
Guanosine analog in the pyrido[2,3-d]pyrimidine ring system as a potential toll-like receptor agonist.
吡啶并[2,3 - d]嘧啶环系统中的鸟苷类似物作为一种潜在的Toll样受体激动剂。
Nucleosides Nucleotides Nucleic Acids. 2006;25(12):1391-7. doi: 10.1080/15257770600918912.
4
New potential inhibitors of cyclin-dependent kinase 4: design and synthesis of pyrido[2,3-d]pyrimidine derivatives under microwave irradiation.细胞周期蛋白依赖性激酶4的新型潜在抑制剂：微波辐射下吡啶并[2,3-d]嘧啶衍生物的设计与合成
Bioorg Med Chem Lett. 2006 Jul 1;16(13):3578-81. doi: 10.1016/j.bmcl.2006.03.084. Epub 2006 Apr 18.
5
Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P(1)(') group.
Bioorg Med Chem Lett. 2004 May 3;14(9):2141-5. doi: 10.1016/j.bmcl.2004.02.033.
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