91639-30-4Relevant academic research and scientific papers
Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2
Wang, Zhen,Zhang, Yali,Pinkas, Daniel M.,Fox, Alice E.,Luo, Jinfeng,Huang, Huocong,Cui, Shengyang,Xiang, Qiuping,Xu, Tingting,Xun, Qiuju,Zhu, Dongsheng,Tu, Zhengchao,Ren, Xiaomei,Brekken, Rolf A.,Bullock, Alex N.,Liang, Guang,Ding, Ke,Lu, Xiaoyun
, p. 7977 - 7990 (2018/09/06)
Discoidin-domain receptors 1 and 2 (DDR1 and DDR2) are new potential targets for anti-inflammatory-drug discovery. A series of heterocycloalkynylbenzimides were designed and optimized to coinhibit DDR1 and DDR2. One of the most promising compounds, 5n, ti
Palladium-Catalyzed Alkylation with Alkyl Halides by C(sp3)?H Activation
Wu, Zhuo,Ma, Ding,Zhou, Bo,Ji, Xiaoming,Ma, Xiaotian,Wang, Xiaoling,Zhang, Yanghui
supporting information, p. 12288 - 12291 (2017/09/06)
Utilizing halogens as traceless directing goups represents an attractive strategy for C?H functionalization. A two C?H alkylation system, initiated by the oxidative addition of organohalides to Pd0, has been developed. The first reaction involves an intermolecular alkylation of palladacycles to form C(sp3)?C(sp2) bonds followed by C(sp2)?H activation/cyclization to deliver alkylated benzocyclobutenes as the final products. In the second reaction, two C?C bonds are formed by the reaction of palladacycles with CH2Br2, and provides a facile and efficient method for the synthesis of indanes. The alkylated benzocyclobutene products can be transformed into tricyclic hyrocarbons, and the indane derivatives are essential structural motifs in bioactive and odorant molecules.
