35480-52-5Relevant articles and documents
Production method of flecainide
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, (2020/05/01)
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.
Effect of flecainide derivatives on sarcoplasmic reticulum calcium release suggests a lack of direct action on the cardiac ryanodine receptor
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
, p. 2446 - 2459 (2016/11/18)
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.
Process for the preparation of 2,5-bis-(2,2,2-trifluoroethoxy)-N-(2-piperidylmethyl)-benzamide and salts thereof
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Page/Page column 7, (2008/12/04)
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.
