13573-28-9Relevant academic research and scientific papers
Nickel-Catalyzed Esterification of Amides Under Mild Conditions
Li, Jun-Fei,Wang, Yao-Fang,Wu, Yuan-Yuan,Liu, Wen-Jing,Wang, Jun-Wen
, p. 874 - 880 (2019/11/13)
Abstract: The use of ligands to adjust the catalytic activity of the catalyst for esterification of amides is challenge in organic chemistry. In this paper, Nickel(II)-NHC-catalyzed the esterification reaction between N,N-di-Boc amide and alcohols at room temperature have been demonstrated. The imidazolium salt bearing a hydroxyl functionalized side arm showed high effective catalytic activity in the activation of the amide N–C bond in air atmosphere. Graphic Abstract: [Figure not available: see fulltext.].
4-AZAINDOLE COMPOUNDS
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Paragraph 0652-0653; 0686-0687, (2019/07/03)
Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein G, A, R1, R5, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9
Polycyclic Sulfoximines as New Scaffolds for Drug Discovery
Borst, Mark L. G.,Ouairy, Cécile M. J.,Fokkema, Sander C.,Cecchi, Alessandro,Kerckhoffs, Jessica M. C. A.,De Boer, Vincent L.,Van Den Boogaard, Peter J.,Bus, Rutger F.,Ebens, Rijko,Van Der Hulst, Rob,Knol, Joop,Libbers, Rob,Lion, Zhou M.,Settels, Bart W.,De Wever, Ellen,Attia, Khaled A.,Sinnema, Piet-Jan,De Gooijer, Jesse M.,Harkema, Karen,Hazewinkel, Marieke,Snijder, Susan,Pouwer, Kees
supporting information, p. 335 - 343 (2018/05/14)
The design and synthesis of three novel polycyclic scaffolds containing sulfoximines are presented in this work, which exemplify that sulfoximines represent a real opportunity for the discovery of new drug candidates. Additionally, the structures present at least two points of diversification and contain a high level of sp3-character, hence being very interesting 3D scaffolds. The compounds synthesized were added to the compound collection of the European Lead Factory.
Diverse ring opening of thietanes and other cyclic sulfides: An electrophilic aryne activation approach
Zheng, Tianyu,Tan, Jiajing,Fan, Rong,Su, Shuaisong,Liu, Binbin,Tan, Chen,Xu, Kun
supporting information, p. 1303 - 1306 (2018/02/14)
Organosulfides are a common class of structure units in bioactive molecules and functional materials motivating continuous developments of efficient synthetic methods. Herein, we report an electrophilic aryne-activated ring opening protocol of one or two
SUBSTITUTED PHENYLOXAZOLIDINONES FOR ANTIMICROBIAL THERAPY
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Page/Page column 40; 42; 138, (2017/02/09)
The present invention relates to novel oxazolidinones (Formula I): or a pharmaceutically acceptable salt having ring A characterized by N-containing monocyclic, bicyclic or spirocyclic substituents, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments.
SUBSTITUTED BICYCLIC AZA-HETEROCYCLES AND ANALOGUES AS SIRTUIN MODULATORS
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Paragraph 0877; 0878, (2017/04/04)
Provided herein are novel substituted bicyclic aza-heterocycle sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents
Gadekar, Pradip K.,Roychowdhury, Abhijit,Kharkar, Prashant S.,Khedkar, Vijay M.,Arkile, Manisha,Manek, Hardik,Sarkar, Dhiman,Sharma, Rajiv,Vijayakumar,Sarveswari
, p. 475 - 487 (2016/07/19)
The design, synthesis and antimicrobial evaluation of a novel series of azaspiro analogues of linezolid (1) have been described. Linezolid comprises of a morpholine ring which is known for its metabolism-related liabilities. Therefore, the key modificatio
Design, synthesis and biological evaluation of paclitaxel-mimics possessing only the oxetane D-ring and side chain structures
Chen, Xing-Xiu,Gao, Feng,Wang, Qi,Huang, Xing,Wang, Dan
, p. 111 - 115 (2014/01/06)
Two spiro paclitaxel-mimics consisting only of an oxetane D-ring and a C-13 side chain were designed and synthesized on the basis of analysis of structure-activity relationships (SAR) of paclitaxel. In vitro microtubule-stabilizing and antiproliferative assays indicated a moderate weaker activity of the mimics than paclitaxel, but which still represented the first example of simplified paclitaxel analogues with significant anti-tumor biological activity.
SUBSTITUTED BICYCLIC AZA-HETEROCYCLES AND ANALOGUES AS SIRTUIN MODULATORS
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Page/Page column 211; 212, (2013/05/09)
Provided herein are novel substituted bicyclic aza-heterocycle sirtuin- modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin- modulating compound in combination with another therapeutic agent.
THIAZOLOPYRIMIDINE COMPOUNDS
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Page/Page column 83, (2012/10/08)
The present invention relates to the use of novel pyrrolopyrazine derivatives of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
