101104-43-2Relevant articles and documents
Pd-Catalyzed Remote Site-Selective and Stereoselective C(Alkenyl)-H Alkenylation of Unactivated Cycloalkenes
Mao, Chun-Li,Zhao, Sheng,Zang, Zhong-Lin,Xiao, Lin,Zhou, Cheng-He,He, Yun,Cai, Gui-Xin
, p. 774 - 787 (2020)
A palladium-catalyzed alkenylation involving remote δ-position C(alkenyl)-H activation of cycloalkenes reacting with electron-deficient alkenes is described. This method features excellent site selectivity and stereoselectivity to efficiently afford only E-selective highly substituted 1,3-diene derivatives with extra-ligand-free and good functional group tolerance including estrone and free N-H tryptamine under weakly alkaline conditions. Mechanistic studies suggest that picolinamide as a bidentate directing group enables the formation of unique alkenyl palladacycle intermediates.
Aryl amide small-molecule inhibitors of microRNA miR-21 function
Naro, Yuta,Thomas, Meryl,Stephens, Matthew D.,Connelly, Colleen M.,Deiters, Alexander
supporting information, p. 4793 - 4796 (2015/10/28)
MicroRNAs (miRNAs) are single stranded RNA molecules of ~22 nucleotides that negatively regulate gene expression. MiRNAs are involved in fundamental cellular processes, such as development, differentiation, proliferation, and survival. MiRNA misregulation has been linked to various human diseases, most notably cancer. MicroRNA-21 (miR-21), a well-established oncomiR, is significantly overexpressed in many types of human cancers, thus rendering miR-21 a potential therapeutic target. Using a luciferase-based reporter assay under the control of miR-21 expression, a high-throughput screen of >300,000 compounds led to the discovery of a new aryl amide class of small-molecule miR-21 inhibitors. Structure-activity relationship (SAR) studies resulted in the development of four aryl amide derivatives as potent and selective miR-21 inhibitors. The intracellular levels of various miRNAs in HeLa cells were analyzed by qRT-PCR revealing specificity for miR-21 inhibition over other miRNAs. Additionally, preliminary mechanism of action studies propose a different mode of action compared to previously reported miR-21 inhibitors, thus affording a new chemical probe for future studies.
Synthesis of 3,4,5,6,7,8-hexahydro-1-substituted phenyl isoquinoline and 3,4,5,6,7,8-hexahydro-1-substituted benzyl isoquinoline
Borthakur, Susanta Kr.,Goswami, Birendra N.
, p. 1045 - 1047 (2008/09/21)
Isoquinoline derivatives are obtained from amides using AlCl3-KI in acetonitrile solvent. This cyclo dehydrating Lewis acid produced no side product and yield is above 95% isoquinoline derivative at room temperature.