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Lacidipine, SN-305, GX-1048, GR-43659X, Viapres, Caldine, Mo

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摘 要：Lacidipine, SN-305, GX-1048, GR-43659X, Viapres, Caldine, Motens, Lacipil, Lacirex,103890-78-4,C26-H33-N-O6,(E)-4-[2-[2-(tert-Butoxycarbonyl)vinyl]phenyl]-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid diethyl ester
  • 【药物名称】Lacidipine, SN-305, GX-1048, GR-43659X, Viapres, Caldine, Motens, Lacipil, Lacirex
  • 【化学名】(E)-4-[2-[2-(tert-Butoxycarbonyl)vinyl]phenyl]-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid diethyl ester
  • 【CAS登记号】103890-78-4
  • 【结构式】Lacidipine, SN-305, GX-1048, GR-43659X, Viapres, Caldine, Mo--药物合成数据库
  • 【分子式】C26-H33-N-O6
  • 【分子量】455.556
  • 【原研厂家】GlaxoSmithKline (Originator), Boehringer Ingelheim (Licensee), Zambon (Licensee)
  • 【作用类别】CARDIOVASCULAR DRUGS, Hypertension, Treatment of, Calcium Channel Blockers
  • 【研发状态】Launched-1991
  • 【合成情况】　
  • 〖来源〗Drugs Fut
  • 〖合成路线〗
  • 〖标题〗LACIDIPINE < Rec INN; BAN; USAN >
  • 〖合成方法〗The Wittig condensation of o-phthalaldehyde (I) with tert-butyl triphenylphosphoranylideneacetate (II) in methylene chloride gives tert-butyl 3-(2-formylphenyl)-2(E)-propenoate (III), which is then cyclized with ethyl 3-aminocrotonate (IV) in acetic acid.
  • 〖作者〗Prous, J.; Castaer, J.
  • 〖参考〗Prous, J.; Castaer, J.; LACIDIPINE Rec INN; BAN; USAN >. Drugs Fut 1989, 14, 4, 317
  • 〖出处〗Drugs Fut1989,14,(4):317
  • 〖备注〗The Wittig condensation of o-phthalaldehyde (I) with tert-butyl triphenylphosphoranylideneacetate (II) in methylene chloride gives tert-butyl 3-(2-formylphenyl)-2(E)-propenoate (III), which is then cyclized with ethyl 3-aminocrotonate (IV) in acetic acid (1). Description Crystals, m.p. 173-5?(1). Manufacturer Glaxo SpA (Italy). References 1. Semeraro, C., Micheli, D., Pieraccioli, D., Gaviraghi, G. and Barthwick, A.D. (Glaxo SpA). 3,5-Pyridinedicarboxylic acid derivatives, process for preparing them and pharmaceutical compositions containing them. AU 8546576, DE 3529997, ES 8703839, ES 8707930, ES 8707931, ES 8707932, ES 8802497, FR 2569402, GB 2164336.
  • 〖来源〗ES 8703839; ES 8703839; US 4801599; US 5011848
  • 〖合成路线〗
  • 〖标题〗1,4-dihydropyridines.
  • 〖合成方法〗The Wittig condensation of o-phthalaldehyde (I) with tert-butyl triphenylphosphoranylideneacetate (II) in methylene chloride gives tert-butyl 3-(2-formylphenyl)-2(E)-propenoate (III), which is then cyclized with ethyl 3-aminocrotonate (IV) in acetic acid.
  • 〖作者〗Borthwick, A.D.; Pierccioli, D.; Micheli, D.; Semeraro, C.; Gaviraghi, G. (Glaxo SpA)
  • 〖参考〗Borthwick, A.D.; Pierccioli, D.; Micheli, D.; Semeraro, C.; Gaviraghi, G. (Glaxo SpA); 1,4-dihydropyridines.. ES 8703839; ES 8703839; US 4801599; US 5011848
  • 〖出处〗ES 8703839; ES 8703839; US 4801599; US 5011848,,():
  • 〖备注〗
 
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