新产品编号:682351
Chemical Name: 4'-Amidino-N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]-2'-methylbiphenyl-4-carboxamide
CAS No. 256227-71-1
项目整合开发状态: Preclinical
项目研究机构: Merck KGaA (Originator)
合成路线:Coupling of 4-bromobenzoyl chloride (I) with amine (II) by means of Et3N in CH2Cl2 or THF yields bromo derivative (III),which is then converted into boronic acid derivative (IV) by treatment with triisopropyloxyboron and n-BuLi in THF/hexane.Suzuki reaction between (IV) and oxadiazole (V) by means of Pd(PPd3)4 and Na2CO3 in dimethoxyethane (DME)/H2O affords compound (VI),which is finally hydrogenated over Raney-Ni in H2O/MeOH/AcOH to furnish the desired product.
📌 参考资料/链接：
参考文献标题:Biphenyl derivs.
文献作者:Van Amsterdam,C.; Harting,J.; Wikstr鰉,H.V.; Liao,Y.; B鰐tcher,H.(Merck Patent GmbH)
参考来源:WO 0005225
📄 详细内容
合成路线:Coupling of 4-bromobenzoyl chloride (I) with amine (II) by means of Et3N in CH2Cl2 or THF yields bromo derivative (III),which is then converted into boronic acid derivative (IV) by treatment with triisopropyloxyboron and n-BuLi in THF/hexane.Suzuki reaction between (IV) and oxadiazole (V) by means of Pd(PPd3)4 and Na2CO3 in dimethoxyethane (DME)/H2O affords compound (VI),which is finally hydrogenated over Raney-Ni in H2O/MeOH/AcOH to furnish the desired product.
参考文献标题:New selective and potent 5-HT1B/1D antagonists: Chemistry and pharmacological evaluation of N-piperazinylphenyl biphenylcarboxamides and biphenylsulfonamides
文献作者:Liao,Y.; B鰐tcher,H.; Harting,J.; Greiner,H.; van Amsterdam,C.; Cremers,T.; Sundell,S.; M鋜z,J.; Rautenberg,W.; Wikstrom,H.
参考来源:J Med Chem 2000,43(3),517
产品链接: CAS No. 256227-71-1››