当前位置: 首页 » 资料 » 药物合成路线 » OKY-1581,,C16-H14-N-O2.Na,2-Methyl-3-[4-(3-pyridinylmethyl)p

OKY-1581,,C16-H14-N-O2.Na,2-Methyl-3-[4-(3-pyridinylmethyl)p

放大字体  缩小字体 更新日期：2018-11-23  浏览次数：365
摘 要：OKY-1581,,C16-H14-N-O2.Na,2-Methyl-3-[4-(3-pyridinylmethyl)phenyl]-2(E)-propenoic acid sodium salt
  • 【药物名称】OKY-1581
  • 【化学名】2-Methyl-3-[4-(3-pyridinylmethyl)phenyl]-2(E)-propenoic acid sodium salt
  • 【CAS登记号】
  • 【结构式】OKY-1581,,C16-H14-N-O2.Na,2-Methyl-3-[4-(3-pyridinylmethyl)p--药物合成数据库
  • 【分子式】C16-H14-N-O2.Na
  • 【分子量】275.2816
  • 【原研厂家】
  • 【作用类别】
  • 【研发状态】Not Determined
  • 【合成情况】　
  • 〖来源〗Drugs Fut
  • 〖合成路线〗
  • 〖标题〗OKY-1581
  • 〖合成方法〗The reaction of 3-chloromethylpyridine (I) with the Grignard reagent of 4-bromobenzaldehyde diethylacetal (II) in THF gives 4-(3-pyridylmethyl)benzaldehyde diethylacetal (III), which is hydrolyzed with aqueous 1N HCl to 4-(3-pyridylmethyl)benzaldehyde (IV). The Wittig condensation of (IV) with 1-(ethoxycarbonyl)ethylidenetriphenylphosphorane (V) in CHCl3 affords 3-[4-(3-pyridylmethyl)phenyl]-2-methylacryl ic acid ethyl ester (VI), which is finally hydrolyzed with aqueous NaOH.
  • 〖作者〗Hillier, K.; Serradell, M.N.; Blancafort, P.; Castaer, J.
  • 〖参考〗Hillier, K.; Serradell, M.N.; Blancafort, P.; Castaer, J.; OKY-1581. Drugs Fut 1982, 7, 6, 399
  • 〖出处〗Drugs Fut1982,7,(6):399
  • 〖备注〗Synthesis of OKY-1581 (EN: 070087) The reaction of 3-chloromethylpyridine (I) with the Grignard reagent of 4-bromobenzaldehyde diethylacetal (II) in THF gives 4-(3-pyridylmethylbenzaldehyde diethylacetal (III), which is hydrolyzed with aqueous 1N HCl to 4-(3-pyridylmethyl)benzaldehyde (IV). The Wittig condensation of (IV) with 1-(ethoxycarbonyl)ethylidenetriphenylphosphorane (V) in CHCl3 affords 3-[4-(3-pyridylmethyl)phenyl]-2-methylacryl ic acid ethyl ester (VI), which is finally hydrolyzed with aqueous NaOH (1). (Scheme 07008701a) Description HCl salt, m.p. 178-80?(1). Manufacturers Ono Pharm. Co., Ltd. (Japan); Kissei Pharm. Co., Ltd. (Japan). Reference 1. Tanouchi, T. et al. (Ono Pharm. Co., Ltd.; Kissei Pharm. Co., Ltd.); US 4271170.
  • 〖来源〗DE 2951786; FR 2445319; FR 2510108; GB 2039903; US 4271170; US 4317828
  • 〖合成路线〗
  • 〖标题〗Pyridine derivatives
  • 〖合成方法〗The reaction of 3-chloromethylpyridine (I) with the Grignard reagent of 4-bromobenzaldehyde diethylacetal (II) in THF gives 4-(3-pyridylmethyl)benzaldehyde diethylacetal (III), which is hydrolyzed with aqueous 1N HCl to 4-(3-pyridylmethyl)benzaldehyde (IV). The Wittig condensation of (IV) with 1-(ethoxycarbonyl)ethylidenetriphenylphosphorane (V) in CHCl3 affords 3-[4-(3-pyridylmethyl)phenyl]-2-methylacryl ic acid ethyl ester (VI), which is finally hydrolyzed with aqueous NaOH.
  • 〖作者〗Tanouchi, T.; et al.
  • 〖参考〗Tanouchi, T.; et al.; Pyridine derivatives. DE 2951786; FR 2445319; FR 2510108; GB 2039903; US 4271170; US 4317828
  • 〖出处〗DE 2951786; FR 2445319; FR 2510108; GB 2039903; US 4271170; US 4317828,,():
  • 〖备注〗
 
本文导航：
  • (1) OKY-1581,,C16-H14-N-O2.Na,2-Methyl-3-[4-(3-pyridinylmethyl)p
 

 

 
推荐图文
益母草 菊花
百合花 西洋参
推荐资料
热门关注