首页> 外国专利> New procedure for resolution of enantiomers (3,4 - Dimethoxy - BICYCLO 4.2.0 octa - 1,3,5 - triennium 2008-2010 - 7 - il) Nitrile and application in the synthesis of Ivabradine

New procedure for resolution of enantiomers (3,4 - Dimethoxy - BICYCLO 4.2.0 octa - 1,3,5 - triennium 2008-2010 - 7 - il) Nitrile and application in the synthesis of Ivabradine

机译:拆分对映异构体的新方法(3,4-二甲氧基-BICYCLO [4.2.0] octa-1,3,5-三年期2008-2010-7-il)腈及其在合成伊伐布雷定中的应用

摘要

Refers to a process of optical resolution (3,4 - Dimethoxy - BICYCLO [4.2.0] octa - 1,3,5 - triennium 2008-2010 - 7 - il) in which separates the Nitrile compound in its two enantiomers by Chiral Chromatography,Where the procedure uses the multi Separation columns or continuous simulated Moving Bed Chromatography at a temperature of 15C to 40oC) stationary Phase which comprises a Silica Gel impregnated with a polysaccharide such as Cellulose or derivative functionalized amilosico t RIS (4 - metilbenzoato) or tris (3,5 - dimetilfenilcarbamato); and (b) that includes isopropanol Mobile phase is recycled, an organic Solvent such as hexane or heptane, or a mixture of both, respectively, at a ratio of 50: 50 2: 98. Also refers to a procedure for the synthesis of Ivabradine that uses the (S) - enantiomer (3,4 - Dimethoxy - BICYCLO [4.2.0] octa - 1,3,5 - triennium 2008-2010 - 7 - il) Nitrile obtained Optical resolution
机译:指光学拆分过程(3,4-二甲氧基-BICYCLO [4.2.0] octa-1,3,5-三年期2008-2010-7-il),其中通过手性色谱分离其两个对映异构体中的腈化合物在此程序中使用多分离柱或在15°C至40°C的温度下进行连续模拟移动床色谱)固定相,该固定相包含硅胶浸渍的多糖,例如纤维素或衍生化的功能化AMIOSICO T RIS(4- metilbenzoato)或tris (3,5-双美芬太尼卡马托); (b)包括异丙醇的流动相以50:50:2:98的比例循环使用,分别以己烷或庚烷之类的有机溶剂或两者的混合物进行再循环。还涉及合成Ivabradine的方法使用(S)-对映异构体(3,4-二甲氧基-BICYCLO [4.2.0]八-1,3,5-三年期2008-2010-7-il)腈光学分辨率

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