开发了新型2-烷基取代的4-氨基咪唑并[1,2- a ][1,3,5]三嗪的高选择性、一锅法、三组分合成方法。该方法的范围在两个维度上进行了探索,改变了三烷基原酸酯和2-氨基咪唑在与氰胺反应中的结构。该方法在微波辐射下方便地进行,在传统加热下也被证明是有效的。使用这种多组分方法制备了高纯度的 24 种新型化合物库。使用 X 射线晶体学研究了代表性分子的分子和晶体结构。
Microwave-assisted synthesis of substituted 2-amino-1H-imidazoles from imidazo[1,2-a]pyrimidines
摘要:
An efficient method for the synthesis of mono- and disubstituted 2-amino-1H-imidazoles via microwave-assisted hydrazinolysis of substituted imidazo[1,2-a]pyrimidines is reported. This protocol avoids strong acidic conditions and is superior to the classical cyclocondensation of alpha-haloketones with N-acetylguanidine. (C) 2009 Elsevier Ltd. All rights reserved.
[EN] 5-HT2B RECEPTOR ANTAGONISTS<br/>[FR] ANTAGONISTES DU RECEPTEUR 5-HT2B
申请人:PHARMAGENE LAB LTD
公开号:WO2005012263A1
公开(公告)日:2005-02-10
Compounds of formulae: (I), (II), (IIIa), (IIIb), (IVa) and (IVb): or a pharmaceutically acceptable salt thereof, for use as pharmaceuticals, in particular for the treatment of a condition alleviated by antagonism of a 5-HT2B receptor.
[EN] INHIBITION OF BACTERIAL BIOFILMS WITH IMIDAZOLE-PHENYL DERIVATIVES<br/>[FR] INHIBITION DE BIOFILMS BACTÉRIENS PAR DES DÉRIVÉS D'IMIDAZOLE-PHÉNYLE
申请人:UNIV NORTH CAROLINA STATE
公开号:WO2009123753A1
公开(公告)日:2009-10-08
Disclosure is provided for imidazole-phenyl derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.
A multicomponent reaction of 2-aminoimidazoles: microwave-assisted synthesis of novel 5-aza-7-deaza-adenines
作者:Felicia Phei Lin Lim、Szy Teng Low、Elvina Lee King Ho、Nathan R. Halcovitch、Edward R. T. Tiekink、Anton V. Dolzhenko
DOI:10.1039/c7ra11305f
日期:——
An efficient and highly selective multicomponent synthesis of 4-aminoimidazo[1,2-a][1,3,5]triazines, which are 5-aza-7-deaza-isosteres of adenine, was developed. The reaction of 2-aminoimidazoles, triethyl orthoformate and cyanamide under microwave irradiation proceeded regioselectively to provide a library of novel 5-aza-7-deaza-adenines in good yields and purity. The developed method was demonstrated
开发了一种高效,高选择性的4-氨基咪唑并[1,2- a ] [1,3,5]三嗪的多组分合成方法,该化合物是腺嘌呤的5-aza-7-deaza-isosteres。2-氨基咪唑,原甲酸三乙酯和氰酰胺在微波辐射下的反应选择性进行,从而以良好的收率和纯度提供了新型5-氮杂-7-脱氮杂戊烯的文库。事实证明,所开发的方法在三种不同的单模微波反应堆中具有可扩展性和高度可重复性。提出了重排以解释反应的高选择性。
5-Ht2b Receptor Antagonists
申请人:Borman Richard Anthony
公开号:US20090018150A1
公开(公告)日:2009-01-15
Compounds of formulae: (I), (II), (IIIa), (IIIb), (IVa) and (IVb): or a pharmaceutically acceptable salt thereof, for use as pharmaceuticals, in particular for the treatment of a condition alleviated by antagonism of a 5-HT
2B
receptor.
INHIBITION OF BACTERIAL BIOFILMS WITH IMIDAZOLE-PHENYL DERIVATIVES
申请人:Melander Christian
公开号:US20090270475A1
公开(公告)日:2009-10-29
Disclosure is provided for imidazole-phenyl derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.