CAS: 2438-32-6; (Z)-But-2-Enedioic Acid,(3S)-3-(4-Chlorophenyl)-N,N-Dimethyl-3-Pyridin-2-Ylpropan-1-Amine

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CAS号113-92-8 扑尔敏

扑尔敏置于β-环糊精体系中,用 Aq. Phosphate Buffer 用作溶剂,化学反应生成马来酸右氯苯那敏,(-)-2-(4-氯-Alpha-(2-(二甲基氨基)乙基)苄基)-吡啶马来酸盐(1:1)
参考文献:β-环糊精开管毛细管电色谱柱的制备及其在十种碱性药物对映体分离中的应用.
标题:β-环糊精开管毛细管电色谱柱的制备及其在十种碱性药物对映体分离中的应用.
摘要:采用(3-巯基丙基)三甲氧基硅烷预衍生化将β-环糊精修饰的金纳米颗粒化学固定在新表面上,制备了开管毛细管电色谱柱.通过透射电子显微镜,扫描电子显微镜,红外光谱和紫外可见光谱对合成的纳米粒子和制备的柱进行了表征.当该柱用作手性固定相时,十种模型碱性药物没有观测到对映选择性.因此,将β-环糊精作为手性添加剂添加到背景电解质中,以期望可能发生协同效应并导致更好的分离.幸运的是,十对药物对映体的对映选择性得到了显着改善.然后,研究了β-环糊精浓度和背景电解质ph对手性分离的影响.采用所开发的分离模式,对佐匹克隆,马来酸氯苯那敏,马来酸溴苯那敏,盐酸二氧丙嗪,卡维地洛的所有对映体(文拉法辛除外)进行了基线分离,分辨率分别为 4.49,1.68,1.88,1.57,2.52,2.33,3.24,1.63 和 3.90分别为氢溴酸后马托品,甲基溴后马托品,文拉法辛,盐酸西布曲明和硫酸特布他林.此外,还讨论了所涉及的可能的分离机制.
Doi:10.1371/journal.Pone.0146292

专利信息

专利号:US-9045788-B2
优先权日:2012-07-17
标题:Process for the enzymatic synthesis of (7S)-1-(3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl) N-methyl methanamine, and application in the synthesis of ivabradine and salts thereof
发明人：PEDRAGOSA-MOREAU SANDRINE; LEFOULON FRANÇOIS; MORIS VARAS FRANCISCO; GONZALEZ SABIN JAVIER
权利人:SERVIER LAB
摘要:Process for the enzymatic synthesis of the compound of formula (I), (7S)-1-(3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl)N-methyl methanamine: n nand application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid.

专利号:US-6906046-B2
优先权日:2000-12-22
标题 :Pharmaceutical uses and synthesis of benzobicyclooctanes
发明人：JACKSON RANDY W; DARWISH IHAB; BAUGHMAN TED A; HOWBERT J JEFFRY
权利人:CELLTECH R & D INC
摘要:Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.

专利号:US-2014024088-A1
优先权日:2012-07-17
标 题:Process for the enzymatic synthesis of (7s)-1-(3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl) n-methyl methanamine, and application in the synthesis of ivabradine and salts thereof

专利号:CA-2820192-C
优先权日:2012-07-17
标 题:Enzymatic synthesis process for (7s)-1-(3,4-dimethoxy bicyclo[4.2.0]octa-1,3,5-triene 7-yl) n-methyl methanamine, and application to the synthesis of ivabradine and of its salts

专利号:CA-2820192-A1
优先权日:2012-07-17
标题:Enzymatic synthesis process for (7s)-1-(3,4-dimethoxy bicyclo[4.2.0]octa-1,3,5-triene 7-yl) n-methyl methanamine, and application to the synthesis of ivabradine and of its salts

专利号:BR-102013017550-A2
优先权日:2012-07-17
标 题:(7s) -1- (3,4-Dimethoxy bicyclo [4. 2.0] octa-1,3,5-triene 7-yl) n-methyl methanamine enzymatic synthesis process and application to the synthesis of ivabradine and of its salts