- Production method of flecainide
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The invention belongs to the technical field of compound synthesis, and particularly relates to a production method of flecainide, which comprises the following steps: 1) etherification reaction, 2) acetylation reaction, 3) oxidation reaction and 4) refining. According to the production method, qualified flecainide is synthesized through three steps, the process steps are simplified, the process operation is simple, the etherification reaction, the acetylation reaction and the oxidation reaction are adopted, so that the flecainide yield is stable, the yield is high, the impurity separation iseasily achieved, and the impurity operation is simple and convenient.
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- Preparation method of 2,5 - di (2,trifluoroethoxy) benzoic acid (by machine translation)
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The invention relates to the field of synthesis of flecainide intermediates, in particular to 2,5 -(2,trifluoroethoxy) benzoic acid is prepared 2,5 - by reacting 2,5 - dihalogenated benzoic acid and trifluoroethanol, and a copper complex serving as a catalyst is further added in the reaction system. The preparation method provided by the invention reduces the reaction temperature. (by machine translation)
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Paragraph 0026-0043; 0045
(2020/12/14)
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- Effect of flecainide derivatives on sarcoplasmic reticulum calcium release suggests a lack of direct action on the cardiac ryanodine receptor
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Background and Purpose: Flecainide is a use-dependent blocker of cardiac Na+channels. Mechanistic analysis of this block showed that the cationic form of flecainide enters the cytosolic vestibule of the open Na+channel. Flecainide is also effective in the treatment of catecholaminergic polymorphic ventricular tachycardia but, in this condition, its mechanism of action is contentious. We investigated how flecainide derivatives influence Ca2+-release from the sarcoplasmic reticulum through the ryanodine receptor channel (RyR2) and whether this correlates with their effectiveness as blockers of Na+and/or RyR2 channels. Experimental Approach: We compared the ability of fully charged (QX-FL) and neutral (NU-FL) derivatives of flecainide to block individual recombinant human RyR2 channels incorporated into planar phospholipid bilayers, and their effects on the properties of Ca2+sparks in intact adult rat cardiac myocytes. Key Results: Both QX-FL and NU-FL were partial blockers of the non-physiological cytosolic to luminal flux of cations through RyR2 channels but were significantly less effective than flecainide. None of the compounds influenced the physiologically relevant luminal to cytosol cation flux through RyR2 channels. Intracellular flecainide or QX-FL, but not NU-FL, reduced Ca2+spark frequency. Conclusions and Implications: Given its inability to block physiologically relevant cation flux through RyR2 channels, and its lack of efficacy in blocking the cytosolic-to-luminal current, the effect of QX-FL on Ca2+sparks is likely, by analogy with flecainide, to result from Na+channel block. Our data reveal important differences in the interaction of flecainide with sites in the cytosolic vestibules of Na+and RyR2 channels.
- Bannister, Mark L,Alvarez-Laviada, Anita,Thomas, N Lowri,Mason, Sammy A,Coleman, Sharon,du Plessis, Christo L,Moran, Abbygail T,Neill-Hall, David,Osman, Hasnah,Bagley, Mark C,MacLeod, Kenneth T,George, Christopher H,Williams, Alan J
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p. 2446 - 2459
(2016/11/18)
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- A practical ligand-free copper(I) bromide-catalyzed fluoroalkoxylation of unactivated aryl bromides
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An efficient ligand-free fluoroalkoxylation of unactivated aryl bromides has been developed, with special attention focused on practicability of the reaction. Without precious metal and organic ligand, the reaction was carried out under the catalytic system of inexpensive copper(I) bromide as a catalyst, N,N-dimethyl formamide as a cocatalyst, and the corresponding stoichiometric sodium fluoroalkoxide as a nucleophilic reagent. The facile approach avoids the drawbacks associated with cost, separation and pollution of ligand to enable sustainable access to aryl fluoroalkyl ethers from readily available bromoarenes.
- Guo, Ying,Li, Yu-Dao,Chen, Cheng,Zhao, Jian-Hong,Liu, Hong-Wei,Liao, Dao-Hua,Ji, Ya-Fei
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p. 2525 - 2537
(2016/03/16)
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- Process for the preparation of 2,5-bis-(2,2,2-trifluoroethoxy)-N-(2-piperidylmethyl)-benzamide and salts thereof
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A process for the preparation of Flecainide acetate, its salts, in particular its pharmaceutically acceptable salts, and intermediates thereof is described wherein 2,5-dibromotoluene is used as a starting material. The method involves a technique for preparing the starting material 2,5-bis(2,2,2-trifluroethoxy)toluene in high yields by reacting 2,5-dibromotoluene with 2,2,2-trifluoroethanol in the presence of a base and a copper-containing catalyst.
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Page/Page column 7
(2008/12/04)
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- Novel process for the preparation of flecainide, its pharmaceutically acceptable salts and important intermediates thereof
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Process for the preparation of Flecainide, its pharmaceutically acceptable salts and important intermediates thereof that involves the use of the 2-halobenzoic acid and its derivatives as a starting material. The use of this process also allows for the synthesis of a novel intermediate useful in the production of Flecainide. This new process is an inexpensive and efficient process for the manufacture of these compounds.
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Page/Page column 4
(2010/02/11)
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- Method for the production of trifluoroethoxy-substituted benzoic acids
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The invention relates to a method for the production of trifluoroethoxy-substituted benzoic acids, by reaction of a corresponding halogenated benzoic acid with trifluoroethanol in the solvent tetrahydrofuran, in the presence of a base and a copper salt, followed by an acidic work-up.
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- Process for the preparation of (2,2,2-trifluoroethoxy)benzoic acids
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A process for producing trifluoroethoxybenzoic acids or salts thereof by reaction of halobenzoic acids or salts thereof with 2,2,2-trifluoroethanol in the presence of a strong base and copper containing materials. The compounds obtained by the process of the present invention may be used as synthetic intermediates in the pharmaceutical industry.
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