POLYCYCLIC QUINAZOLINES, PREPARATION THEREOF, AND USE THEREOF
申请人:Li Jianqi
公开号:US20110288086A1
公开(公告)日:2011-11-24
At least one active pharmaceutical ingredient is chosen from polycyclic quinazolines of formula V,
pharmaceutically acceptable salts thereof, and hydrates of the pharmaceutically acceptable salts. The active pharmaceutical ingredients disclosed may be inhibitors of protein tyrosine kinase inhibitors and/or aurora kinase. The active pharmaceutical ingredients can be used for treating cancers susceptible to treatment with protein tyrosine kinase inhibitors and/or aurora kinase inhibitors.
The purpose of the present invention is to provide a compound having excellent antibacterial activity against
mycobacterium tuberculosis
, multidrug-resistant tuberculosis bacteria, and/or non-tuberculous acid-fast bacteria. A compound represented by formula [I]:
(in the formula, each symbol is as described in the attached specification), or a salt thereof can be used to diagnose, prevent, and/or treat tuberculosis.
Construction of a Benzo[<i>b</i>]azepine Skeleton through Decarboxylative Ylide [6+1] Annulations with Modified Vinyl Benzoxazinanones
作者:Qing-Zhu Li、Zhi-Qiang Jia、Lin Chen、Xiang Zhang、Hai-Jun Leng、Rong Zeng、Yan-Qing Liu、Wen-Lin Zou、Jun-Long Li
DOI:10.1021/acs.orglett.0c04041
日期:2021.2.5
A Lewis acid-promoted [6+1] annulation between sulfur ylides and modified vinyl benzoxazinanones was described. In this reaction, the newly designed vinyl benzoxazinanones could serve as a novel six-atom synthon, and the key to success is the installation of an electron-withdrawing group on the alkene moiety of the benzoxazinanones. A broad range of substrates are compatible with this mild reaction
描述了路易斯酸促进硫基化物和改性乙烯基苯并恶嗪酮之间的[6 + 1]环化。在该反应中,新设计的乙烯基苯并恶嗪酮可以用作新型的六原子合成子,成功的关键是在苯并恶嗪酮的烯烃部分上安装了一个吸电子基团。各种各样的底物都与这种温和的反应体系兼容,从而为构建苯并[ b ]氮杂骨架提供了简便实用的方法。
N-Heterocyclic-Carbene-Catalyzed Synthesis of 2-Aryl Indoles
作者:M. Todd Hovey、Christopher T. Check、Alexandra F. Sipher、Karl A. Scheidt
DOI:10.1002/anie.201405035
日期:2014.9.1
A convergent and efficient transition‐metal‐free catalytic synthesis of 2‐aryl‐indoles has been developed. The interception of a highly reactive and transient aza‐ortho‐quinonemethide by an acyl anion equivalent generated through N‐hetereocyclic carbene catalysis is central to this successful strategy. High yields and a wide scope as well as the streamlined synthesis of a kinase inhibitor are reported
Phosphine-Catalyzed Reaction between 2-Aminobenzaldehydes and Dialkyl Acetylenedicarboxylates: Synthesis of 1,2-Dihydroquinoline Derivatives and Toward the Development of an Olefination Reaction
reacting 2-aminobenzaldehyde derivatives and dialkyl acetylenedicarboxylates with catalytic amounts of phosphine. This reaction was rendered catalytic by the selective in situ phosphine oxide reduction with the use of phenylsilane. Furthermore, with the same starting materials and with an additional role of the reducing agent, a new olefination reaction was discovered. Hydrogen/deuterium (H/D) exchange