[EN] QUINOLINE AND QUINAZOLINE COMPOUNDS<br/>[FR] COMPOSÉS QUINOLÉINE ET QUINAZOLINE
申请人:ACERTA PHARMA BV
公开号:WO2016055982A1
公开(公告)日:2016-04-14
In some embodiments, the invention relates to quinazoline and quinoline compounds of Formula I: (I) or a pharmaceutically acceptable salt thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, in some embodiments, the present invention relates to quinazoline and quinoline compounds, pharmaceutical compositions thereof, and the use of the compounds and pharmaceutical compositions in the treatment of Bruton's tyrosine kinase (BTK) mediated disorders.
The series of derivatives of substituted N-pyridinylsalicylamides were synthesized. The compounds were evaluated for in vitro antimycobacterial activity against Mycobacterium avium and two strains of Mycobacterium kansasii. In the quantitative structure activity relationships analysis (QSAR), the Free-Wilson and Hansch approaches were used but the analysis was not significant. (The standard deviations
Trifluoroacetic Acid-Mediated Denitrogenative <i>ortho</i>-Hydroxylation of 1,2,3-Benzotriazin-4(3<i>H</i>)-ones: A Metal-Free Approach
作者:Kanagaraj Madasamy、Madasamy Hari Balakrishnan、Ramaraju Korivi、Subramaniyan Mannathan
DOI:10.1021/acs.joc.2c00354
日期:2022.7.1
An efficient trifluoroacetic acid-mediated denitrogenative hydroxylation of 1,2,3-benzotriazin-4(3H)-ones is described. This metal-free approach is compatible with a wide range of 1,2,3-benzotriazin-4(3H)-ones, affording ortho-hydroxylated benzamides in good to high yields with a short reaction time. The reaction is believed to proceed via a benzene diazonium intermediate. The synthetic utility of
描述了一种有效的三氟乙酸介导的 1,2,3-benzotriazin-4(3 H )-ones 的脱氮羟基化。这种不含金属的方法与多种 1,2,3-benzotriazin-4(3 H )-one相容,可在较短的反应时间内以良好至高产率提供邻羟基化苯甲酰胺。据信该反应通过苯重氮中间体进行。该反应的合成效用通过以良好收率制备抗微生物药物利肝素 C 和苯并恶嗪-2,4(3 H )-二酮类化合物得到成功证明。
Chaaban, I.; El-Kersh, M. A., Pharmazie, 1984, vol. 39, # 3, p. 183 - 184