发明名称 Procedure for obtaining 3-isopropyl-5-(2'-methoxy)ethyl 2,6-dimethyl-4-(3'-nitrophenyl)-1,4-dihydropyridine-3,5- dicarboxylate
摘要 New procedure for obtaining 3-isopropyl-5-(2'- methoxy)ethyl 2,6-dimethyl-4-(3'-nitrophenyl)-1,4- dihydropyridine-3,5-dicarboxylate, in three stages. The obtaining of isopropyl 2-(3'-nitro)benzylidene- acetoacetate from 3-nitrobenzaldehyde and isopropyl acetoacetate in the presence of piperidine, glacial acetic acid and isopropanol. A second step in which 2- methoxyethyl 3-aminocrotonate is obtained by treating 2- methoxyethyl acetoacetate with ammonium acetate. In the third step the products obtained previously are treated in the presence of activated alumina to give the title product. Advantages which are obtained relative to the prior art: a) Processes carried out under rapid, smooth and simple conditions, giving products of high quality. b) The time is reduced in the last step. c) The last step is carried out in a solid phase, avoiding traces of symmetrical dihydropyridines. d) Obtaining of the dihydropyridine without a solvent, minimum production of contaminating effluent. e) Use of recyclable basic or acid catalysts. f) Low cost by the minimization of reagents and residues. <IMAGE>
申请公布号 ES2055653(A1) 申请公布日期 1994.08.16
申请号 ES19920001891 申请日期 1992.09.22
申请人 ELMUQUIMICA FARMACEUTICA, S.L. 发明人 BURGOS GARCIA CAROLINA;IZQUIERDO CEINOS MARIA LUISA;GARCIA NAVIO JOSE LUIS;VAQUERO LOPEZ JUAN JOSE;ALVAREZ-BUILLA GOMEZ JULIO;NOVELLA ROBISCO JOSE LUIS;CALATAYUD ARINERO JOSE;MONTORO JIMENEZ ANTONIO F.
分类号 A61K31/44;C07D211/90;(IPC1-7):C07D211/90 主分类号 A61K31/44
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