92663-22-4Relevant academic research and scientific papers
PAd2-DalPhos Enables the Nickel-Catalyzed C?N Cross-Coupling of Primary Heteroarylamines and (Hetero)aryl Chlorides
Clark, Jillian S. K.,Ferguson, Michael J.,McDonald, Robert,Stradiotto, Mark
supporting information, p. 6391 - 6395 (2019/04/08)
Base-metal catalysts capable of enabling the assembly of heteroatom-dense molecules by cross-coupling of primary heteroarylamines and (hetero)aryl chlorides, while sought-after given the ubiquity of unsymmetrical di(hetero)arylamino fragments in pharmacophores, are unknown. Herein, we disclose the new “double cage” bisphosphine PAd2-DalPhos (L2). The derived air-stable NiII pre-catalyst C2 functions well at low loadings in challenging test C?N cross-couplings with established substrates, and facilitates the first Ni-catalyzed C?N cross-couplings of primary five- or six-membered ring heteroarylamines and activated (hetero)aryl chlorides, with synthetically useful scope that is competitive with Pd catalysis.
NEUROPROTECTIVE COMPOSITIONS AND METHODS OF USING THE SAME
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Paragraph 00162-00163; 00187-00193, (2019/12/04)
This invention is directed to neuroprotective compositions and methods of using the same to treat neurodegenerative diseases.
Synthesis and evaluation of the 2-aminothiazoles as anti-tubercular agents
Kesicki, Edward A.,Bailey, Mai A.,Ovechkina, Yulia,Early, Julie V.,Alling, Torey,Bowman, Julie,Zuniga, Edison S.,Dalai, Suryakanta,Kumar, Naresh,Masquelin, Thierry,Hipskind, Philip A.,Odingo, Joshua O.,Parish, Tanya
, (2016/06/01)
The 2-aminothiazole series has anti-bacterial activity against the important global pathogen Mycobacterium tuberculosis. We explored the nature of the activity by designing and synthesizing a large number of analogs and testing these for activity against M. tuberculosis, as well as eukaryotic cells. We determined that the C-2 position of the thiazole can accommodate a range of lipophilic substitutions, while both the C-4 position and the thiazole core are sensitive to change. The series has good activity against M. tuberculosis growth with sub-micromolar minimum inhibitory concentrations being achieved. A representative analog was selective for mycobacterial species over other bacteria and was rapidly bactericidal against replicating M. tuberculosis. The mode of action does not appear to involve iron chelation. We conclude that this series has potential for further development as novel antitubercular agents.
COMPOUNDS AND METHODS FOR INDUCING BROWNING OF WHITE ADIPOSE TISSUE
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Page/Page column 12; 15; 18, (2016/09/15)
The present invention provides a compound for inducing browning of white adipose tissue in vitro and in vivo of formula I, the preparation method thereof, as well as a composition comprising the same. Further, the present invention also relates to the use of the compound and the method to treat metabolic disorders, such as obesity and diabetes.
Direct preparation of thiazoles, imidazoles, imidazopyridines and thiazolidines from alkenes
Donohoe, Timothy J.,Kabeshov, Mikhail A.,Rathi, Akshat H.,Smith, Ian E. D.
experimental part, p. 1093 - 1101 (2012/04/04)
A range of heterocycles, namely thiazoles, imidazoles, imidazopyridines, thiazolidines and dimethoxyindoles, have been synthesised directly from alkenes via a two-step ketoidoination/cyclisation protocol. The alkene starting materials are themselves readily accessible using many different and well-established approaches, and allow access to a variety of heterocycles with excellent yields and regioselectivity.
