423740-50-5Relevant academic research and scientific papers
Benzoic acid derivative as well as preparation method and medicinal application thereof
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, (2021/09/21)
The invention discloses a benzoic acid derivative as well as a preparation method and a pharmaceutical application thereof, and belongs to the technical field of medicines. The invention specifically discloses a benzoic acid derivative represented by a co
Visible light-promoted copper catalyzed regioselective acetamidation of terminal alkynes by arylamines
Pampana, V. Kishore Kumar,Sagadevan, Arunachalam,Ragupathi, Ayyakkannu,Hwang, Kuo Chu
supporting information, p. 1164 - 1170 (2020/03/11)
Herein, we describe a copper photoredox catalyzed synthesis of acetamide via regioselective C-N coupling of arylamines with terminal alkynes using molecular oxygen (O2) as an oxidant at room temperature under visible light irradiation (47 examples). Unique simultaneous formation of both amide and ester functionalities occurs via intramolecular cyclization in a single-step reaction in the case of anthranilic acids using inexpensive copper as a catalyst and eco-friendly O2 as an oxidant and reagent. Different substrates undergo different reaction pathways to generate similar acetamide products, as evidenced by 18O2 labelling experiments. The current protocol was also applied for the rapid, few step preparation of biologically active inhibitors (BACE-1 and PDE4). This process can be readily scaled up to a gram scale, and calculations of green metrics suggest the economic feasibility and eco-friendly nature of the current photoredox approach.
Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK
Hom, Roy K.,Bowers, Simeon,Sealy, Jennifer M.,Truong, Anh P.,Probst, Gary D.,Neitzel, Martin L.,Neitz, R. Jeffrey,Fang, Larry,Brogley, Louis,Wu, Jing,Konradi, Andrei W.,Sham, Hing L.,Tóth, Gergely,Pan, Hu,Yao, Nanhua,Artis, Dean R.,Quinn, Kevin,Sauer, John-Michael,Powell, Kyle,Ren, Zhao,Bard, Frédérique,Yednock, Ted A.,Griswold-Prenner, Irene
scheme or table, p. 7303 - 7307 (2011/02/22)
From high throughput screening, we discovered compound 1, the prototype for a series of disubstituted thiophene inhibitors of JNK which is selective towards closely related MAP kinases p38 and Erk2. Herein we describe the evolution of these compounds to a novel class of thiophene and thiazole JNK inhibitors that retain favorable solubility, permeability, and P-gp properties for development as CNS agents for treatment of neurodegeneration. Compound 61 demonstrated JNK3 IC50 = 77 nM and retained the excellent broad kinase selectivity observed for the series.
