Sarpogrelate hydrochloride, MCI-9042, Anplag
盐酸沙格雷酯 沙格雷酯 Chemical Name: Succinic acid (?-1-(dimethylaminomethyl)-2-[2-[2-(3-methoxyphenyl)ethyl]phenoxy]ethyl monoester hydrochloride
CAS No. 135159-51-2, 125926-17-2 (free base)
项目整合开发状态: Launched-1993
项目研究机构: Mitsubishi Pharma (Originator)
合成路线:The reaction of 2-hydroxy-3'-methoxybibenzyl (I) with epichlorohydrin (II) by means of NaH in DMF gives 2-(2,3-epoxypropoxy)-3'-methoxybibenzyl (III),which by reaction with dimethylamine in refluxing THF yields 2-[3-(dimethylamino)-2-hydroxypropoxy]-3'-methoxybibenzyl (IV).Finally,this compound is treated with succinic anhydride (V) in refluxing THF and with HCl in acetone.
📌 参考资料/链接：
参考文献标题:Pharmaceutically active (3-aminopropoxy)-bibenzyl derivs
文献作者:Kikumoto,R.; Fukami,H.; Hara,H.; Ninomiya,K.; Sugano,M.(Mitsubishi Chemical Corp.)
参考来源:EP 0072942
📄 详细内容
合成路线:The reaction of 2-hydroxy-3'-methoxybibenzyl (I) with epichlorohydrin (II) by means of NaH in DMF gives 2-(2,3-epoxypropoxy)-3'-methoxybibenzyl (III),which by reaction with dimethylamine in refluxing THF yields 2-[3-(dimethylamino)-2-hydroxypropoxy]-3'-methoxybibenzyl (IV).Finally,this compound is treated with succinic anhydride (V) in refluxing THF and with HCl in acetone.
参考文献标题:Syntheses and platelet aggregation inhibitory and antithrombotic properties of [2-[(omega-aminoalkoxy)phenyl]ethyl]benzenes
文献作者:Osakabe,M.; Fukami,H.; Sugano,M.; Kikumoto,R.; Ninomiya,K.; Tamao,Y.; Hara,H.
参考来源:J Med Chem 1990,33(6),1818
合成路线:The reaction of 2-hydroxy-3'-methoxybibenzyl (I) with epichlorohydrin (II) by means of NaH in DMF gives 2-(2,3-epoxypropoxy)-3'-methoxybibenzyl (III),which by reaction with dimethylamine in refluxing THF yields 2-[3-(dimethylamino)-2-hydroxypropoxy]-3'-methoxybibenzyl (IV).Finally,this compound is treated with succinic anhydride (V) in refluxing THF and with HCl in acetone.
参考文献标题:Sarpogrelate Hydrochloride
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1992,17(12),1093
产品链接: CAS No. 135159-51-2›› 产品链接: CAS No.125926-17-2››