Dexrazoxane, ADR-529, NSC-169780, ICRF-187(HCl)
右雷佐生Chemical Name: (+)-(S)-4,4'-(Propane-1,2-diyl)bis(piperazine-2,6-dione)
CAS No. 24584-09-6
项目整合开发状态: Not Determined
项目研究机构: Cancer Research UK (Originator)
合成路线:(rac)-1,2-Diaminopropane is resolved using (-)-L-tartaric acid.The bitartrate salt is treated with HCl to give the dihydrochloride salt,(-)-S-1,2-diaminopropane dihydrochloride (I).(I) in water is added to a solution of chloroacetic acid and sodium hydroxide below 20 C,and allowed to stand at room temperature for 7 days.After concentration and filtration,the product is isolated by passing the filtrate down an ion exchange column and eluting with water.The portion of the eluate containing the bulk of the optical activity is concentrated by heating.Crystals of (+)-(S)-1,2-propylene dinitrilotetraacetic acid (II) are obtained by filtration.(II) is heated under nitrogen for 20 h at 165 C to give (+)-(S)-1,2-di(piperazine-2,6-dione)propane.
📌 参考资料/链接：
参考文献标题:ICRF-187
文献作者:Eastland,G.
参考来源:Drugs Fut 1987,12(11),1017
📄 详细内容
合成路线:(rac)-1,2-Diaminopropane is resolved using (-)-L-tartaric acid.The bitartrate salt is treated with HCl to give the dihydrochloride salt,(-)-S-1,2-diaminopropane dihydrochloride (I).(I) in water is added to a solution of chloroacetic acid and sodium hydroxide below 20 C,and allowed to stand at room temperature for 7 days.After concentration and filtration,the product is isolated by passing the filtrate down an ion exchange column and eluting with water.The portion of the eluate containing the bulk of the optical activity is concentrated by heating.Crystals of (+)-(S)-1,2-propylene dinitrilotetraacetic acid (II) are obtained by filtration.(II) is heated under nitrogen for 20 h at 165 C to give (+)-(S)-1,2-di(piperazine-2,6-dione)propane.
参考文献标题:NS-2330 enters phase IIb in Alzheimer's disease
文献作者:
参考来源:J Pharm Sci 1976,65238-242
产品链接: CAS No. 24584-09-6››