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项目整合精选>>>Masnidipine hydrochloride, Lercanidipine hydrochloride, TJN-324, Rec-15/2375, Lercan, Cardiovasc, Lerzam, Zanidip, Lerdip, Lercadip, Zanedip
Masnidipine hydrochloride, Lercanidipine hydrochloride, TJN-324, Rec-15/2375, Lercan, Cardiovasc, Lerzam, Zanidip, Lerdip, Lercadip, Zanedip
盐酸乐卡地平 乐卡地平 Chemical Name: (?-1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)pyridine-3,5-dicarboxylic acid 2-[N-(3,3-diphenylpropyl)-N-methylamino]-1,1-dimethylethyl methyl diester hydrochloride
CAS No. 132866-11-6, 100427-26-7 (free base)
项目整合开发状态: Launched-1997
项目研究机构: Recordati (Originator), Asta Medica (Licensee), Dainippon Pharmaceutical (Licensee), Forest (Licensee), Kwizda (Licensee), Napp (Licensee), Rotta (Licensee), Tsumura (Licensee), UCB (Licensee), Uriach (Licensee), Zambon (Licensee), Eurand (Formulation), L
合成路线:Two new related ways for the synthesis of lercanidipine have been reported:1) The condensation of diketene (I) with the aminoalcohol (II) gives the corresponding acetoacetate ester (III),which is allowed to react with 3-nitrobenzaldehyde (IV) by means of HCl in chloroform yielding the expected benzylidene derivative (V).Finally,this compound is cyclized with methyl 3-aminocrotonate (VI) in refluxing isopropanol.2) By esterification of 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid monomethyl ester (VIII) with alcohol (II) by means of SOCl2 in DMF/dichloromethane.
📌 参考资料/链接：
参考文献标题:N-(3,3-diphenylpropyl)aminoethylesters of 1,4-dihydro-2,6-dimethylpyridine-3,5-dicarboxylic acid,compositions and use
文献作者:Nardi,D.; Leonardi,A.; Graziani,G.; Bianchi,G.(Recordati Industria Chimica e Farmaceutica SpA)
参考来源:EP 0153016; JP 60199874; US 4772621; US 4968832
📄 详细内容
合成路线:Two new related ways for the synthesis of lercanidipine have been reported:1) The condensation of diketene (I) with the aminoalcohol (II) gives the corresponding acetoacetate ester (III),which is allowed to react with 3-nitrobenzaldehyde (IV) by means of HCl in chloroform yielding the expected benzylidene derivative (V).Finally,this compound is cyclized with methyl 3-aminocrotonate (VI) in refluxing isopropanol.2) By esterification of 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid monomethyl ester (VIII) with alcohol (II) by means of SOCl2 in DMF/dichloromethane.
参考文献标题:REC 15/2375
文献作者:Bianchi,G.; Leonardi,A.
参考来源:Drugs Fut 1987,12(12),1113
合成路线:Two new related ways for the synthesis of lercanidipine have been reported:1) The condensation of diketene (I) with the aminoalcohol (II) gives the corresponding acetoacetate ester (III),which is allowed to react with 3-nitrobenzaldehyde (IV) by means of HCl in chloroform yielding the expected benzylidene derivative (V).Finally,this compound is cyclized with methyl 3-aminocrotonate (VI) in refluxing isopropanol.2) By esterification of 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid monomethyl ester (VIII) with alcohol (II) by means of SOCl2 in DMF/dichloromethane.
参考文献标题:Asymmetric N-(3,3-diphenylpropyl)aminoalkyl esters of 4-aryl-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acids with antihypertensive activity
文献作者:Catto,A.; Motta,G.; Pennini,R.; Testa,R.; Sironi,G.; Cerri,A.; Leonardi,A.
参考来源:Eur J Med Chem 1998,33(5),399
产品链接: CAS No. 132866-11-6›› 产品链接: CAS No.100427-26-7››