611-35-8Relevant articles and documents
Highly Chemoselective Deoxygenation of N-Heterocyclic N-Oxides Using Hantzsch Esters as Mild Reducing Agents
An, Ju Hyeon,Kim, Kyu Dong,Lee, Jun Hee
supporting information, p. 2876 - 2894 (2021/02/01)
Herein, we disclose a highly chemoselective room-temperature deoxygenation method applicable to various functionalized N-heterocyclic N-oxides via visible light-mediated metallaphotoredox catalysis using Hantzsch esters as the sole stoichiometric reductant. Despite the feasibility of catalyst-free conditions, most of these deoxygenations can be completed within a few minutes using only a tiny amount of a catalyst. This technology also allows for multigram-scale reactions even with an extremely low catalyst loading of 0.01 mol %. The scope of this scalable and operationally convenient protocol encompasses a wide range of functional groups, such as amides, carbamates, esters, ketones, nitrile groups, nitro groups, and halogens, which provide access to the corresponding deoxygenated N-heterocycles in good to excellent yields (an average of an 86.8% yield for a total of 45 examples).
QUINOLINE-BASED COMPOUNDS AND METHODS OF INHIBITING CDK8/19
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Paragraph 0108; 0117-0118; 0123, (2020/03/09)
Disclosed herein are quinoline-based compounds and method for inhibiting CDK8 or CDK19 for the intervention in diseases, disorders, and conditions. The quinoline-based composition comprise substituents at quinoline ring positions 4 and 6, wherein the substituent at position 4 is selected from a substituted or unsubstituted arylalkylamine or a substituted or unsubstituted arylhetrocyclylamine. Pharmaceutical compositions comprising the substituted qunioline compositions, methods of inhibiting CDK8 or CDK19, and methods of treating CDK8/19-associated diseases, disorders, or conditions are also disclosed.
Derivative containing aromatic ring/aromatic heterocycle-triazole-methylene-TCP and preparation method and application thereof
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Paragraph 0061; 0064, (2020/08/09)
The invention discloses a derivative containing aromatic ring/aromatic heterocycle-triazole-methylene-TCP, which has a structure shown in a general formula I, has remarkable biological inhibition activity on LSD1, can be used for preparing a medicine for inhibiting LSD1, enriches the variety of TCP derivatives, and lays a foundation for researching and developing a novel LSD1 inhibitor. Particularly, the derivative can be used for preparing anti-tumor medicines, has a certain inhibition effect on a plurality of tumor cell strains such as gastric cancer cell strains (MGC-803, SGC-7901), breastcancer cell strains (MCF-7) and prostate cancer cell strains (PC-3), shows antitumor activity, provides a lead compound structure for anticancer drugs, and has a good application prospect. The invention also provides a preparation method of the aromatic ring/aromatic heterocycle-triazole-methylene-TCP containing derivative, (1R, 2S)-phenylcyclopropylamine or (1R, 2S)-3, 4-difluorophenylcyclopropylamine is used as a raw material, the derivative is prepared through alkyne feeding and cycloaddition reactions, the preparation method is simple, and batch production and commercial application are facilitated.