1818-28-6Relevant articles and documents
Compound for treating or preventing hepatopathy (by machine translation)
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Paragraph 0253-0254; 0256, (2019/10/01)
The invention discloses a compound, an optical isomer or a pharmaceutically acceptable salt, an optical isomer or a pharmaceutically acceptable salt thereof for treating or preventing hepatopathy, and the compound, optical isomer or pharmaceutically acceptable salt thereof can be applied to the preparation of a medicine for treating or preventing liver diseases. (by machine translation)
A new efficient method for the preparation of intermediate aromatic ketones by Friedel–Crafts acylation
Jin, Xiaojun,Wang, Ailing,Cao, Hongyu,Zhang, Shujia,Wang, Lihao,Zheng, Xueliang,Zheng, Xuefang
, p. 5521 - 5530 (2018/04/30)
Abstract: As the most important method to prepare pharmaceutical and chemical intermediate aromatic ketones, Friedel–Crafts (F–C) acylation is used to seek a novel catalytic system which is imminently consistent with the concept of green chemistry. In this study, six deep eutectic solvents (DES) were synthesized for the Friedel–Crafts acylation reaction as a catalytic solvent. Among the six DES, choline chloride-zinc chloride ([ChCl][ZnCl2]2) proved to be the most competent candidate of electron-rich arenes with acylation reagent. It got the highest yield when 1.0 equivalent of [ChCl][ZnCl2]2 used with acyl halides at 70?°C. Recycled DES was reused directly without any extra process. After five cycles, the catalytic activity did not decrease significantly (80–85%). Finally, according to experimental validation, the possible mechanism of this reaction was considered. Graphical Abstract: [Figure not available: see fulltext.].
Hexafluoro-2-propanol-Promoted Intermolecular Friedel-Crafts Acylation Reaction
Vekariya, Rakesh H.,Aubé, Jeffrey
supporting information, p. 3534 - 3537 (2016/08/16)
The intermolecular Friedel-Crafts acylation was carried out in hexafluoro-2-propanol to yield aryl and heteroaryl ketones at room temperature without any additional reagents.
Trimethoxy-chalcone derivatives inhibit growth of Leishmania braziliensis: Synthesis, biological evaluation, molecular modeling and structure-activity relationship (SAR)
Bello, Murilo Lamim,Chiaradia, Louise Domeneghini,Dias, Luiza Rosaria Sousa,Pacheco, Leticia Kramer,Stumpf, Taisa Regina,Mascarello, Alessandra,Steindel, Mario,Yunes, Rosendo Augusto,Castro, Helena Carla,Nunes, Ricardo Jose,Rodrigues, Carlos Rangel
scheme or table, p. 5046 - 5052 (2011/09/30)
In this work we described the synthesis, the antileishmanial activity and the molecular modeling and structure-activity relationship (SAR) evaluations of a series of chalcone derivatives. Among these compounds, the methoxychalcones 2h, 2i, 2j, 2k and 2l showed significant antileishmanial activity (IC 50 50 = 2.7 μM), 2j (IC50 = 3.9 μM) and 2k (IC50 = 4.6 μM) derivatives presented better antileishmanial activity than the control drug pentamidine (IC50 = 6.0 μM). Our SAR study showed the importance of methoxy di-ortho substitution at phenyl ring A and the relationship between the frontier orbital HOMO coefficients distribution of these molecules and their activity. The most active compounds 2h, 2i, 2j, 2k, and 2l fulfilled the Lipinski rule-of-five which theoretically is important for good drug absorption and permeation through biological membranes. The potential profile of 2j (IC 50 = 3.9 μM and CC50 = 216 μM) pointed this chalcone derivative as a hit compound to be further explored in antileishmanial drug design.
One-pot two-step oxidative cleavage of 1,2-arylalkenes to aryl ketones instead of arylaldehydes in an aqueous medium: A complementary approach to ozonolysis
Sharma, Naina,Sharma, Abhishek,Kumar, Rakesh,Shard, Amit,Sinha, Arun K.
supporting information; experimental part, p. 6025 - 6032 (2011/02/23)
A new approach has been developed for a one-pot and selective oxidative cleavage of aryl- and 1,2-diarylalkenes leading to one-carbon shorter aryl ketones; thereby, providing a complementary approach to classical ozonolysis. The methodology was applicable to diverse aromatic and polyaromaticarylalkenes bearing electron-donating or -withdrawing groups on the aromatic ring. The protocol also provided a useful one-pot oxidative cleavage-condensation sequence, which could potentially have important applications in natural product total synthesis. A one-pot, two-step approach has been achieved for the oxidative cleavage of 1,2-disubstituted arylalkenes into the corresponding aryl ketones instead of arylaldehydes (see scheme; NIS = N-iodosuccinimide; CTAB = cetyltrimethylammonium bromide; PDC/TBHP = pyridinium dichromate/tert-butyl hydroperoxide). The methodology also led to a valuable one-pot oxidative cleavage-condensation reaction that has widespread utility in the total synthesis of natural products.
Synthesis of aryl ketones by palladium(II)-catalyzed decarboxylative addition of benzoic acids to nitriles
Lindh, Jonas,Sjoeberg, Per J. R.,Larhed, Mats
supporting information; experimental part, p. 7733 - 7737 (2011/01/05)
An efficient, sustainable method for the preparation of aryl ketones from ortho-substituted benzoic acids proceeds through their decarboxylation to generate an aryl-palladium species, followed by addition to a nitrile and hydrolysis of the intermediate ketimine.
Synthesis and hypolipidemic activity of modified side chain α-asarone homologues
Cruz,Garduno,Salazar,Martinez,Jimenez-Vazquez,Diaz,Chamorro,Tamariz
, p. 535 - 544 (2007/10/03)
A series of homologues of α-asarone (1), containing variable size and functionality on the side chain attached to the aromatic ring, has been subjected to a study of structure-activity relationship. For most of the prepared derivatives, either with a carbonyl (8a-8e), a hydroxy group (9a-9e), or with a conjugated double bond (10a-10d), significant effects on serum lipoprotein cholesterol, LDL-cholesterol, HDL-cholesterol and triglycerides were displayed. The results showed an enhancement of the hypocholesterolemic activity as the length of the chain is decreased. Theoretical conformational and electrostatic potential analyses of 1 and olefins 10 suggest unfavorable steric interactions in the bulky superior side-chain homologues as the deactivating biological effect.
4,6-diarylpyrimidine derivatives and salts thereof
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, (2008/06/13)
Described are a 4,6-diarylpyrimidine derivative represented by the following formula (1): STR1 wherein R represents a heterocyclic ring which may be substituted by one to four lower alkyl groups or an amino group and Ar represents a phenyl, naphthyl or ar
Time-resolved fluorescence and transient spectroscopy in determining photochemical and photophysical channels in reacting systems in solutions and microheterogeneous media
Whitten, David G.,Farahat, Mohammad S.,Gaillard, Elizabeth R.
, p. 23 - 32 (2007/10/03)
Characterization of short-lived intermediates in homogeneous and microheterogeneous systems has been carried out using time-resolved spectroscopic techniques. The data obtained from these techniques have been analyzed in a relatively unconventional manner to elucidate complex transient behavior for two reactive systems. The highly nonexponential fluorescence decay for a series of trans-stilbene-derivatized amphiphiles that readily form bilayer systems in aqueous media has been analyzed using a distribution of lifetimes analysis (DLA). The utility of DLA for quantitative studies was first determined by simulation of artificial decay data. Despite some limitations in DLA, qualitative conclusions as to the nature of the fluorescing species may be drawn when supplementary information such as steady-state spectroscopic data are also considered. The results indicate that the observed fluorescence originates from different types of excited- state species that consist of two or more trans-stilbene units; one of the emissions is attributed to the excited state of a ground-state aggregate while the other is assigned to an excimer that may arise from a 'defect' in the bilayer. The nonexponential nature of the decays is attributed to distributions of environments experienced by the fluorescing species. Electron transfer (ET) reactions between several excited pinacols and carbon tetrachloride in solution have been found to yield products with quantum yields that are higher than unity in the presence of oxygen, suggesting a chain mechanism for product formation. In these systems both the donor and the acceptor undergo bond fragmentation following the initial ET step. The individual steps involved in the proposed mechanism fur these systems have been investigated in part using different steady-state and time-resolved laser spectroscopic techniques. However, it was also necessary to utilize pulse radiolysis in order to confirm the involvement of certain radical intermediates that were not observable by the usual flash photolysis techniques.
