7649-92-5Relevant academic research and scientific papers
Method for synthesizing pitavastatin calcium intermediate by microchannel reactor
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Paragraph 0034-0068; 0073-0077, (2021/07/24)
The invention relates to a method for synthesizing a pitavastatin calcium intermediate in a microchannel reactor. Fluorobenzene and phthalic anhydride are used as raw materials, a target product 2-(4-fluoro-benzoyl)-benzoic acid is synthesized through the microchannel reactor, and in the reaction process, and a carbonate compound is used for replacing aluminum trichloride in the prior art to serve as a catalyst, so the catalyst treatment before industrial production is avoided, meanwhile, a large amount of aluminum-containing wastewater is not generated in the reaction process, the method is green and environment-friendly, the reaction condition is mild, the reaction time is short, the product yield is high and reaches 92% or above, the purity is high and reaches 99% or above, the product post-treatment is simple, the cost is reduced, and the method is suitable for industrial production.
Divergent Synthesis of Highly Substituted Pyridines and Benzenes from Dienals, Alkynes, and Sulfonyl Azides
Luo, Han,Li, You,Du, Luan,Xin, Xiaolan,Wang, Tao,Han, Jingpeng,Tian, Yi,Li, Baosheng
supporting information, p. 7883 - 7887 (2021/10/20)
Divergent synthesis is extremely important for the highly efficient preparation of structurally diverse target molecules. Herein, we describe a multicomponent cascade reaction, which allows access to highly substituted pyridines and benzenes by combining four individual steps in a one-pot manner from the same set of readily available starting materials. The azepine intermediates were first used as the precursors for 6π-electrocyclization to construct highly substituted pyridines and benzenes in a tunable manner.
A facile greener synthesis, antimicrobial evaluation and molecular modelling of new 4-aryl-2-(3-(2-(trifluoromethyl)phenyl)-1,8-naphthyridin-2-yl)phthalazin-1(2H)-one derivatives
Sakram, Boda,Ravi, Dharavath,Raghupathi, Mutyala,Kumar, Boda Sathish,Anantha Lakshmi
, p. 2007 - 2022 (2019/01/10)
Abstract: The synthesis of 4-aryl-2-(3-(2-(trifluoromethyl)phenyl)-1,8-naphthyridin-2-yl)phthalazin-1(2H)-ones was performed by cyclization of 2-hydrazinyl-3-(2-(trifluoromethyl)phenyl)-1,8-naphthyridine with 2-aroylbenzoic acids in ethanol containing a catalytic amount of concentrated sulfuric acid under solid state conditions. All these synthesized compounds (8a–h) were screened for their in vitro antibacterial activity against gram-positive bacteria such as (Staphylococcus aureus) and gram-negative bacteria (Escherichia coli) and also evaluated for their antifungal activity against Aspergillus Niger and Helmenthosphorium oryzae fungal strains. Some of the products demonstrate good antibacterial activity and moderate antifungal activity. In predominantly, 8b, 8d, 8g, and 8h compounds showed good to excellent antibacterial and antifungal activities. The antimicrobial activity of the compound 8 was further investigated with the help of in LibDock score docking study to predict the active sites. Graphical abstract: [Figure not available: see fulltext.].
Divergent Access to (1,1) and (1,2)-Azidolactones from Alkenes using Hypervalent Iodine Reagents
Alazet, Sébastien,Le Vaillant, Franck,Nicolai, Stefano,Courant, Thibaut,Waser, Jerome
supporting information, p. 9501 - 9504 (2017/07/22)
A versatile synthesis of azidolactones through azidation and cyclization of carboxylic acids onto alkenes has been developed. Based on either photoredox or palladium catalysis, (1,1) and (1,2) azido lactones can be selectively synthesized. The choice of catalyst and benziodoxol(on)e reagent serving as azide source was essential to initiate either a radical or Lewis acid mediated process with divergent outcome. These transformations were carried out under mild conditions using a low catalyst loading and gave access to a large scope of azido lactones.
Synthesis and Biological Evaluation of New Phthalazinone Derivatives as Anti-Inflammatory and Anti-Proliferative Agents
Hameed, Alhamzah Dh.,Ovais, Syed,Yaseen, Raed,Rathore, Pooja,Samim, Mohammed,Singh, Surender,Sharma, Kalicharan,Akhtar, Mymona,Javed, Kalim
, p. 150 - 159 (2016/02/09)
The chemistry of phthalazine derivatives has been of increasing interest since many of these compounds have found many chemotherapeutic applications. So this study aims to synthesize a library of phthalazine derivatives and to investigate their anti-inflammatory and anti-proliferative activities. Sixteen new phthalazinone derivatives (2a-p) were synthesized and tested for their in vitro antiproliferative and in vivo anti-inflammatory activities. All the synthesized compounds were identified and characterized by IR, 1H NMR, 13C NMR spectroscopy, and MS. Two compounds, 2b and 2i, showed significant anti-inflammatory activity comparable with that of the standard drug etoricoxib in the carrageenan-induced rat paw edema model at 3 and 5 h, respectively. Three compounds (2h, 2j, and 2g) showed moderate sensitivity toward the renal cancer cell line UO-31. A library of new phthalazone compounds (2a-p) was synthesized as dual inhibitors (COX-2/LOX-5) and evaluated for their anti-inflammatory, anticancer activities. Two compounds showed significant anti-inflammatory activity comparable with that of the standard drug etoricoxib, whereas three compounds showed moderate sensitivity toward the renal cancer cell line UO-31.
Palladium-catalyzed chemoselective decarboxylative ortho acylation of benzoic acids with α-oxocarboxylic acids
Miao, Jinmin,Ge, Haibo
supporting information, p. 2930 - 2933 (2013/07/26)
Palladium-catalyzed chemoselective decarboxylative cross coupling of benzoic acids with α-oxocarboxylic acids was realized via an arene sp 2 C-H functionalization process. This work represents the first example of transition-metal-catalyzed cro
Studies on synthetic and structural characterization of new fluorine substituted phthalides of pharmaceutical interest
Chamoli, Tanu,Rawat,Jacob, Melissa
, p. 748 - 757 (2012/10/30)
An efficient and economical synthesis of some new fluorine substituted phthalides was accomplished from two γ-keto acids, 2-(4-fluorobenzoyl) benzoic acid and 2-(3,5-dinitro-4-flurobenzoyl)benzoic acid. Each acid was reacted with various phenolic compounds in presence of catalytic quantity of concentrated sulphuric acid to get the phthalides. The structures of the synthesized compounds were established on the basis of their elemental analysis, spectral data and chemical reactions. Some of the synthesized phthalides exhibited antibacterial and antifungal activity on antimicrobial screening against human pathogenic bacteria and fungi.
PROCESS FOR THE PRODUCTION OF [2- (4-FLUORO-BENZYL) -PHENYL] -ACETIC ACID
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Page/Page column 5; 6, (2008/06/13)
The present invention relates to a novel process for the production of [2-(4-fluoro-benzyl)-phenyl]-acetic acid, a compound obtainable from phthalic anhydride. The process comprises the subsequent steps a) through e): a) reacting phthalic anhydride with fluorobenzene or a derivative thereof in appropriate reaction conditions; b) over reducing the product obtained in step a) at the ketone moiety; c) reducing the product obtained in step b) with sodium dihydro-bis (2- 15 methoxyethoxy) aluminate (Red-Al) to the corresponding alcohol ; d) chlorinat ing the alcohol obtained in step c) ; e) inserting CO into the product obtained in step d) through an appropriate Pd-containing catalytic system. In an alternative embodiment, the step e) is replaced by the steps f1) and f2) : f1) reacting the product obtained in step d) with sodium cyanide ; f2) hydro lysing the product obtained in step f1). The present invention provides a process for the production of [2-(4-fluoro-benzyl)- phenyl]-acetic acid which is suitable for industrial scale reactors (e.g. which is cleaner and more efficient). Also, [2-(4-fluoro-benzyl)-phenyl]-acetic acid is obtained as a crystalline material with a purity > 95%.
Novel N-(3-hydroxy-4-piperidinyl)benzamide derivatives
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, (2008/06/13)
Novel N-(3-hydroxy-4-piperidinyl)benzamides and derivatives thereof, said compounds being useful as stimulators of the motility of the gastro-intestinal system.
N-aryl-piperazinealkanamides useful for protecting hearts from myocardial injury caused by ischaemia, anoxia or hypoxia
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, (2008/06/13)
Novel N-aryl-piperazinealkanamides, having particular substituents attached to one of the carbon atoms of the piperazine ring, which compounds are useful to protect hearts from myocardial injury caused by ischaemia, anoxia or hypoxia.
