53267-01-9Relevant articles and documents
Novel Process For The Preparation Of (-)-Cibenzoline Succinate
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Paragraph 0246; 0247, (2020/08/11)
The present invention relates to a crystalline form of (-)-cibenzoline succinate. The present invention also relates to a method for manufacturing (-)-cibenzoline succinate having a chiral purity of 99.9% or higher. In addition, the present invention provides the method for manufacturing (-)-cibenzoline succinate and a crystalline form thereof. The (-)-cibenzoline succinate according to the present invention is economical and remarkably advantageous for mass production.COPYRIGHT KIPO 2020
Novel process for the synthesis of class I antiarrhythmic agent (±)-cibenzoline and its analogs
Gholap, Atul R.,Paul, Vincent,Srinivasan, Kumar V.
, p. 2967 - 2982 (2008/12/22)
Synthesis of (±)-cibenzoline and its analogs has been achieved by a simple sequence of reactions. The diaryl cyanoolefin intermediate 3 could be prepared by Knoevenagel condensation of benzophenone with ethylcyanoacetate to form the tetra-substituted olefin intermediate 2 followed by Krapcho deethoxycarbonylation or from β-hydroxynitrile intermediate 2' followed by the elimination of hydroxyl group respectively. The 2,2- diphenylcyclopropanecarbonitrile 4 was synthesized from intermediate 3 by cyclopropanation, which was converted to (±)-2-(2,2-diphenylcyclopropyl)- 2-imidazoline 5 by reaction with ethylenediamine in the presence of a catalytic amount of sulfur. Moreover, the obtained 2-imidazolines were smoothly oxidized to the corresponding imidazoles 6 in good to moderate yields. Copyright Taylor & Francis Group, LLC.