YM-461
Chemical Name: 1-(3-Phenylpropyl)-4-[2-(3-pyridyl)thiazolidin-4(R)-ylcarbonyl]piperazine fumarate
项目整合开发状态: Preclinical
项目研究机构: Yamanouchi (Originator)
合成路线:Adamantylbenzoic acid (I) was converted to acid chloride (II) on treatment with SOCl2,and subsequently condensed with allyl p-hydroxybenzoate (III) in the presence of Et3N to afford the benzoyloxybenzoic ester (IV).The allyl ester was then cleaved by refluxing in aqueous ethanol in the presence of tris(triphenylphosphine)rhodium chloride to yield the title compound.
📌 参考资料/链接：
参考文献标题:Aromatic esters and thioesters,process for their preparation and their use in human or animal therapeutics and in cosmetics
文献作者:Shroot,B.; Eustache,J.; Bernardon,J.-M.(CIRD Galderma)
参考来源:AU 8928608; EP 0325540
📄 详细内容
合成路线:Adamantylbenzoic acid (I) was converted to acid chloride (II) on treatment with SOCl2,and subsequently condensed with allyl p-hydroxybenzoate (III) in the presence of Et3N to afford the benzoyloxybenzoic ester (IV).The allyl ester was then cleaved by refluxing in aqueous ethanol in the presence of tris(triphenylphosphine)rhodium chloride to yield the title compound.
参考文献标题:Aromatic esters and thioesters,a process for their preparation and their use in human or veterinary medicine and in cosmetic compsns.
文献作者:Eustache,J.; Bernardon,J.-M.; Shroot,B.(CIRD Galderma)
参考来源:US 5173289