In the presence of equimolar quantity of BCl3, phenols 1 react with isocyanates and acyl chlorides to give, usually with good-excellent yields, 2-hydroxy-aryl-carboxy-amides 2 and 2-hydroxy-aryl-ketones 3 respectively. A distinctive behaviour of BCl3 in comparison with other Lewis acids is observed.
A medicament having inhibitory activity against NF-κB activation, which comprises a compound represented by the following general formula (I) or a pharmacologically acceptable salt as an active ingredient:
wherein X represents a connecting group, A represents hydrogen atom or acetyl group, E represents an aryl group or a heteroaryl group, and ring X represents an arene or a heteroarene.
Inhibitors against the production and release of inflammatory cytokines
申请人:——
公开号:US20040259877A1
公开(公告)日:2004-12-23
A medicament having inhibitory activity against NF-&kgr;B activation, which comprises a compound represented by the following general formula (I) or a pharmacologically acceptable salt as an active ingredient:
1
wherein X represents a connecting group, A represents hydrogen atom or acetyl group, E represents an aryl group or a heteroaryl group, and ring X represents an arene or a heteroarene.
INHIBITORS AGAINST THE PRODUCTION AND RELEASE OF INFLAMMATORY CYTOKINES
申请人:Institute of Medicinal Molecular Design, Inc.
公开号:EP1352650A1
公开(公告)日:2003-10-15
A medicament having inhibitory activity against NF- κ B activation, which comprises a compound represented by the following general formula (I) or a pharmacologically acceptable salt as an active ingredient:
wherein X represents a connecting group, A represents hydrogen atom or acetyl group, E represents an aryl group or a heteroaryl group, and ring X represents an arene or a heteroarene.
一种对 NF-κ B 活化具有抑制活性的药物,其活性成分包括下通式(I)所代表的化合物或药理学上可接受的盐:
其中,X 代表连接基团,A 代表氢原子或乙酰基,E 代表芳基或杂芳基,环 X 代表芳炔或杂芳炔。
One-Pot Synthesis of Salicylanilides by Direct Amide Bond Formation from Salicyclic Acid Under Microwave Irradiation
作者:Cheng-Rong Lu、Bei Zhao、Ying-Peng Jiang、Hao Ding、Sheng Yang
DOI:10.1080/00397911.2010.481745
日期:2011.4.5
[image omitted] A highly efficient protocol for the preparation of aromatic amides is described by the direct reactions between salicyclic acid and aromatic amines in the presence of phosphorous trichloride under microwave irradiation. The method has several advantages over the conventional methods, including operational simplicity, good yield, and reduced reaction time.