合成目标产物 Phthaloyl Amlodipine 主要起始原料 2-Chlorobenzaldehyde And Methyl 3-Aminocrotonate And Ethyl4-[2-(1,3-Dioxo-1,3-Dihydro-2H-Isoindol-2-yl)Ethoxyl]-3-Oxobutanoate
400024-08-0 + 14205-39-1 = 88150-62-3 反应条件:1.1 Solvents: Isopropanol; 12 H,Rt -> Reflux 标题:Synthesis And Structural Identification Of Impurities From Amlodipine Besylate 作者:Zhang,Ya-Lu; Et Al 参考文献:Shenyang Yaoke Daxue Xuebao 日期:2015 卷标:32(3) 页码:188-192]
88150-75-8 = 88150-62-3 反应条件:1.1 Reagents: Ammonium Acetate Solvents: Ethanol; 1 H,Reflux2.1 Solvents: Acetic Acid; 20 H,Reflux 标题:Synthesis Of Amlodipine Besylate 作者:Shi,Weibing; Et Al 参考文献:Zhongguo Yaowu Huaxue Zazhi 日期:2006 卷标:16(3) 页码:161-164]
265136-65-0 = 88150-62-3 反应条件:1.1 Solvents: Acetic Acid; 20 H,Reflux 标题:Synthesis Of Amlodipine Besylate 作者:Shi,Weibing; Et Al 参考文献:Zhongguo Yaowu Huaxue Zazhi 日期:2006 卷标:16(3) 页码:161-164]
专利号:US-6603006-B2 优先权日:1998-10-26 标题:Intermediate for the synthesis of amlodipine, a process for the preparation thereof and corresponding use 发明人:COPPI LAURA; GASANZ GUILLEN YOLANDA; CAMPON PARDO JULIO 权利人:ESTEVE QUIMICA SA 摘要:An intermediate for the synthesis of amlodipine, a process for the preparation thereof and the corresponding use are disclosed. The intermediate is ethyl 3-amino-4-(2-(phthalimido)ethoxy)crotonate and is of formula III:The process for the preparation thereof comprises reacting the acetoacetate of formula:with ammonium acetate; and the use thereof is for the preparation of the compound of formula:the process being conducted by reacting ethyl 3-amino-4-[2-(phthalimido)ethoxy]crotonate with a benzylidene derivative.
专利号:US-7671208-B2 优先权日:2007-03-30 标题 :Acetone solvate of phthaloyl amlodipine 发明人:BERENGUER MAIMO RAMON; MEDRANO RUPEREZ JORGE; MERODIO CABANILLAS JUAN FRANCISCO 权利人:ESTEVE QUIMICA SA 摘要:An acetone solvate of phthaloyl amlodipine, as well as a process for its preparation including dissolving phthaloyl amlodipine in acetone and cooling the mixture. The present invention also comprises a method for the synthesis of amlodipine, its salts or solvates, which comprises the use of an acetone solvate of phthaloyl amlodipine.
专利号:WO-2004058711-A1 优先权日:2002-12-30 标 题 :Isolation of dihydropyridine derivative and preparation salts thereof 发明人:ASLAN TUNCER; ADIYAMAN MUSTAFA; YURDAKUL AYCIL; SAHPAZ FILIZ; OZARSLAN EVREN A; GUNER DIDEM; RIDVANOGLU NURTEN 权利人:EOS ECZACIBASI OZGUN KIMYASAL; ASLAN TUNCER; ADIYAMAN MUSTAFA; YURDAKUL AYCIL; SAHPAZ FILIZ; OZARSLAN EVREN A; GUNER DIDEM; RIDVANOGLU NURTEN 摘要:The title compound is isolated in pure form by using a crystallization process and converted to its pharmaceutically acceptable salts. The crystallization process affects stability and purity of the amlodipine salts. All known impurities and one unknown impurity, which forms during the synthesis of the amlodipine salts, were isolated, characterized, and synthesized. A new method allowing the quantitative HPLC analysis of all related impurities of amlodipine salts in a single chromatogram was developed.
专利号:DE-69929079-T2 优先权日:1998-10-26 标题:INTERMEDIATE FOR THE SYNTHESIS OF AMLODIPIN, METHOD OF MANUFACTURE AND CORRESPONDING APPLICATION
专利号:EP-1125924-B1 优先权日:1998-10-26 标题:Intermediate for the synthesis of amlodipine, preparation process and corresponding utilization
专利号:US-2002068831-A1 优先权日:1998-10-26 标 题 :Intermediate for the synthesis of amlodipine, a process for the preparation there and corresponding use
1: Gottwald-Hostalek U, Sun N, Barho C, Hildemann S. Management of Hypertension With a Fixed-Dose (Single-Pill) Combination of Bisoprolol and Amlodipine. Clin Pharmacol Drug Dev. 2017 Jan;6(1):9-18. doi: 10.1002/cpdd.309. Epub 2016 Oct 26. Review. , Nirmala, M., Babu, J. M., Vyas, K., Reddy, G. M., Bhaskar, B. V., ... & Mukkanti, K. (2006). Identification and characterization of potential impurities of amlodipine maleate. Journal of pharmaceutical and biomedical analysis, 40(3), 605-613.