- NOVEL PROCESS FOR THE PREPARATION OF (+)-CIBENZOLINE SUCCINATE
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The present invention relates to a crystalline form of (+)-Cibenzoline succinate. The present invention is also related to a process for the preparation of (+)-Cibenzoline succinate with chiral purity greater than 99.9%. The present invention also provides a process for the preparation of (+)-Cibenzoline succinate and a crystalline form thereof.
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Paragraph 204-208
(2020/05/12)
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- Novel Process For The Preparation Of (-)-Cibenzoline Succinate
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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
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Paragraph 0220-0222
(2020/08/11)
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- Novel process for the synthesis of class I antiarrhythmic agent (±)-cibenzoline and its analogs
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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.
- Gholap, Atul R.,Paul, Vincent,Srinivasan, Kumar V.
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p. 2967 - 2982
(2008/12/22)
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