新产品编号:43223

Chemical Name: N,N-Dimethyl-N-[2-[(3R,5aS,6R,8aS,9R,10S,12R,12aR)-3,6,9-trimethylperhydro-3,12-epoxypyrano[4,3-j]-1,2-benzodioxepin-10-yloxy]ethyl]amine oxalate; 10beta-[2-(N,N-Dimethylamino)ethyl]-10-deoxoartemisinin oxalate
CAS No. 139716-81-7 (non-specific stereoch.), 139716-80-6 (undefined isomer, free base)
项目整合开发状态: Preclinical
项目研究机构: Academy of Military Medical Sciences (Originator), Shanghai Institute Materia Medica (Originator)
合成路线:Dihydroartemisinin (II) was prepared by NaBH4 reduction of artemisinin (I).Condensation of (II) with 2-bromoethanol (A) in the presence of boron trifluoride etherate yielded the 10beta-bromoethyl acetal (III).Finally,reaction of (III) with dimethylamine in DMF provided the desired amine,which was finally converted to the oxalate salt.
📌 参考资料/链接:
参考文献标题:Synthesis and antimalarial activity of artemisinin derivatives containing an amino group
文献作者:Li,Y.; Zhu,Y.M.; Jiang,H.J.; Pan,J.P.; Wu,G.S.; Wu,J.M.; Shi,Y.L.; Yang,J.D.; Wu,B.A.
参考来源:J Med Chem 2000,43(9),1635