102421-43-2Relevant articles and documents
Synthesis and evaluation of azalamellarin N and its A-ring-modified analogues as non-covalent inhibitors of the EGFR T790M/L858R mutant
Fukuda, Tsutomu,Anzai, Mizuho,Nakahara, Akane,Yamashita, Kentaro,Matsukura, Kazuaki,Ishibashi, Fumito,Oku, Yusuke,Nishiya, Naoyuki,Uehara, Yoshimasa,Iwao, Masatomo
, (2021)
Azalamellarin N, a synthetic lactam congener of the marine natural product lamellarin N, and its A-ring-modified analogues were synthesized and evaluated as potent and non-covalent inhibitors of the drug-resistant epidermal growth factor receptor T790M/L8
An Efficient Coupling of p-Quinone Mono-Imine Ketals and Aryl/Alkyl Thiols: Rapid Synthesis of Biaryl/Aryl–Alkyl Sulfides
Sharma, Arun,Peddinti, Rama Krishna
, p. 2230 - 2237 (2017)
We report a fast, efficient, and metal-free protocol for the synthesis of unsymmetrical biaryl sulfides and aryl–alkyl sulfides (4-methoxy-2-sulfanyl-phenylcarbamates) under catalytic influence of 2,4-dinitrobenzoic acid. The reaction proceeded in a regioselective anti-Michael addition fashion and all the products were obtained within a very short period of time and in good to excellent yields.
FOURTH-GENERATION EGFR TYROSINE KINASE INHIBITOR
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Paragraph 0206-0209, (2021/04/30)
Provided is a compound having a tyrosine kinase inhibitory activity specific to C797S resistant mutant EGFR (particularly C797S tertiary-resistant mutant EGFR) and is useful as a C797S resistant mutant EGFR (particularly C797S mutant tertiary-resistant EG
Metal-free synthesis of fluorinated indoles enabled by oxidative dearomatization
Vitaku, Edon,Smith, David T.,Njardarson, Jon T.
supporting information, p. 2243 - 2247 (2016/02/18)
Nitrogen heterocycles are found in a majority of approved small-molecule pharmaceuticals, and the number of approved fluorinated drugs is increasing each decade. Therefore, new approaches for accessing fluorinated nitrogen heterocycles are of great significance. A novel, scalable, and metal-free method for accessing a wide range of fluorinated indoles is described. This oxidative-dearomatization-enabled approach assembles 2-trifluoromethyl NH-indole products from simple commercially available anilines with hexafluoroacetylacetone in the presence of an organic oxidant. The nature of the aniline N-capping group is critical for the success of this new reaction. Furthermore, the indole products contain a 3-trifluoroacetyl group, which can be exploited to access a plethora of useful functional groups.
Palladium-catalyzed oxidative carbonylation of aromatic C-H bonds of N -alkylanilines with CO and alcohols for the synthesis of o -aminobenzoates
Chen, Ming,Ren, Zhi-Hui,Wang, Yao-Yu,Guan, Zheng-Hui
, p. 1258 - 1263 (2015/01/30)
A Pd(II)-catalyzed C-H monocarbonylation of N-alkylanilines for the synthesis of o-aminobenzoates has been developed. Various aliphatic alcohols and phenol were tolerated in the reaction to afford the corresponding o-aminobenzoates in good yields under mild balloon pressure of CO.
Structure-activity studies in the development of a hydrazone based inhibitor of adipose-triglyceride lipase (ATGL)
Mayer, Nicole,Schweiger, Martina,Melcher, Michaela-Christina,Fledelius, Christian,Zechner, Rudolf,Zimmermann, Robert,Breinbauer, Rolf
, p. 2904 - 2916 (2015/03/30)
Adipose triglyceride lipase (ATGL) catalyzes the degradation of cellular triacylglycerol stores and strongly determines the concentration of circulating fatty acids (FAs). High serum FA levels are causally linked to the development of insulin resistance a
Synthesis of new verapamil analogues and their evaluation in combination with rifampicin against Mycobacterium tuberculosis and molecular docking studies in the binding site of efflux protein Rv1258c
Singh, Kawaljit,Kumar, Malkeet,Pavadai, Elumalai,Naran, Krupa,Warner, Digby F.,Ruminski, Peter G.,Chibale, Kelly
supporting information, p. 2985 - 2990 (2014/06/24)
New verapamil analogues were synthesized and their inhibitory activities against Mycobacterium tuberculosis H37Rv determined in vitro alone and in combination with rifampicin (RIF). Some analogues showed comparable activity to verapamil and exhibited better synergies with RIF. Molecular docking studies of the binding sites of Rv1258c, a M. tuberculosis efflux protein previously implicated in intrinsic resistance to RIF, suggested a potential rationale for the superior synergistic interactions observed with some analogues.
ANTIBACTERIAL COMPOUNDS
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Page/Page column 192, (2013/04/24)
The present Invention relates to cephalosporin antibacterial compounds of Formula (!): corresponding pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods for bacterial infections, especially those caused by gram-negative bacteria.
Axially chiral dicarboxylic acid catalyzed activation of quinone imine ketals: Enantioselective arylation of enecarbamates
Hashimoto, Takuya,Nakatsu, Hiroki,Takiguchi, Yuka,Maruoka, Keiji
supporting information, p. 16010 - 16013 (2013/11/19)
The synthetic utility of quinone imine ketals in the context of asymmetric catalysis was disclosed for the first time. By expanding the utility of chiral Bronsted acid catalysis to the electrophilic activation of quinone imine ketals, we succeeded in the development of highly enantioselective arylation of encarbamates to give α-amino-β-aryl ethers wherein quinone imine ketals act as functionalized aromatic ring surrogate. Further transformations of the products were also examined to establish procedures to provide chiral β-aryl amines and α-aryl esters.
Phosphoramidate tantalum complexes for room-temperature C-H functionalization: Hydroaminoalkylation catalysis
Garcia, Pierre,Lau, Ying Yin,Perry, Mitchell R.,Schafer, Laurel L.
supporting information, p. 9144 - 9148 (2013/09/12)
A cooled reaction: Phosphoramidate-ClTaMe3 complexes promote the first example of room-temperature hydroaminoalkylation catalysis. This reaction can be realized under solvent-free conditions and with challenging substrates such as styrenes and dialkyl amines. When using a vinylsilane substrate, for the first time the linear regioisomer is obtained preferentially using a Group5 metal. TBS=tert-butyldimethylsilyl, TMS=trimethylsilyl. Copyright