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).
Unsymmetrical bisquinolines with high potency against P. falciparum Malaria
Burgess, Steven J.,Gunsaru, Bornface,Kelly, Jane X.,Li, Yuexin,Liebman, Katherine M.,Liebman, Michael C.,Morrill, Westin,Peyton, David H.
, (2020/05/18)
Quinoline-based scaffolds have been the mainstay of antimalarial drugs, including many artemisinin combination therapies (ACTs), over the history ofmoderndrugdevelopment. Althoughmuch progress has beenmade in the search for novel antimalarial scaffolds, itmay be that quinolineswill remain useful, especially if very potent compounds fromthis class are discovered. We report here the results of a structure-activity relationship(SAR) study assessingpotentialunsymmetrical bisquinoline antiplasmodial drug candidates using in vitro activity against intact parasites in cell culture. Many unsymmetrical bisquinolineswere found to be highly potent against both chloroquine-sensitive and chloroquine-resistant Plasmodium falciparum parasites. Further work to develop such compounds could focus on minimizing toxicities in order to find suitable candidates for clinical evaluation.
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.
