3815-63-2Relevant academic research and scientific papers
COMPOSITIONS AND METHODS FOR THE TREATMENT OF CANCER
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Paragraph 0256, (2020/07/08)
This disclosure relates to compounds, pharmaceutical compositions comprising them, and methods of using the compounds and compositions for treating diseases related to Heat Shock Transcription Factor 1 (HSF1) activity and/or function. More particularly, this disclosure relates to methods of inhibiting HSF1 activity with these compounds and pharmaceutical compositions thereof, and methods of treating diseases associated with HSF1 activity and/or function, such as cancer.
Palladium-Catalyzed Synthesis of Symmetrical and Unsymmetrical Ureas Using Chromium Hexacarbonyl as a Convenient and Safe Alternative Carbonyl Source
Mozaffari, Mozhdeh,Nowrouzi, Najmeh
supporting information, p. 7541 - 7544 (2019/12/12)
Pd-catalyzed synthesis of urea derivatives from aryl iodides and different aliphatic and aromatic amines using sodium azide and chromium hexacarbonyl is described. In this process, carbonylation of aryl iodides, Curtius rearrangement of aroyl azides, and nucleophilic addition of amines sequentially occur to afford the products in good to excellent yields. This protocol is operationally simple and displays a broad substrates scope.
Scalable, One-Pot, Microwave-Accelerated Tandem Synthesis of Unsymmetrical Urea Derivatives
Kulkarni, Abhijit R.,Garai, Sumanta,Thakur, Ganesh A.
, p. 992 - 999 (2018/06/18)
We report a facile, microwave-accelerated, one-pot tandem synthesis of unsymmetrical ureas via a Curtius rearrangement. In this method, one-pot microwave irradiation of commercially available (hetero)aromatic acids and amines in the presence of diphenylphosphoryl azide enabled extremely rapid (1-5 min) construction of an array of unsymmetrical ureas in good to excellent yields. We demonstrate the utility of our method in the efficient, gram-scale synthesis of key biologically active compounds targeting the cannabinoid 1 and α7 nicotinic acetylcholine receptors.
Phenyl 4,5-dichloro-6-oxopyridazine-1(6H)-carboxylate as carbonyl source: Facile and selective synthesis of carbamates and ureas under mild conditions
Lee, Hyung-Geun,Kim, Min-Jung,Park, Song-Eun,Kim, Jeum-Jong,Kim, Bo Ram,Lee, Sang-Gyeong,Yoon, Yong-Jin
experimental part, p. 2809 - 2814 (2010/03/03)
The selective syntheses of carbamates, symmetric -ureas, and unsymmetrical ureas have been accomplished by the -reaction of amines with phenyl 4,5-dichloro-6-oxopyridazine-1(6H)-carboxylate as a carbonyl source under mild conditions. It is noteworthy that this process is mild, economic, and convenient.
Kinetics and mechanism of the anilinolysis of S-aryl N-arylthiocarbamates in acetonitrile
Sung, Dae Dong,Jang, Hee Man,Jung, Dae Il,Leeb, Ikchoon
experimental part, p. 1014 - 1019 (2009/10/26)
The aminolysis reactions of S-aryl N-arylthiocarbamates (YC 6H4NH-C(=O)-SC6H4Z, 1) with anilines in acetonitrile are studied. The reaction rates are more influenced by the nucleophilicity of the nucleophile than the nucleofugality of the leaving group, but the change In the effective charge from reactants to the TS for formation of the tetrahedral intermediate is slightly greater in the leaving group (βz from-0.07 to -0.14) than In the nucleophile (βx = 0.04-0.12). The magnitude of the Broensted coefficients are in the range of values that are consistent for a stepwise mechanism with rate-limiting formation of the zwitterionic tetrahedral intermediate. Signs of cross-interaction constants, ρxy (>0), ρxz (>0) and ρyz (0), are all consistent with a stepwise mechanism. It Is concluded that the change of the amine from benzylamines to anilines causes a shift of the aminolysis mechanism from a concerted to a stepwise process. Copyright
DIARYL UREAS AS CB1 ANTAGONISTS
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Page/Page column 38, (2008/06/13)
Compounds of Formula I are provided. In which the variables are as described herein. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies and various in vitro assays.
