Elmustine, NSC-29485, HECNU
依莫司汀Chemical Name: 1-(2-Chloroethyl)-3-(2-hydroxyethyl)nitrosourea
CAS No. 60784-46-5
项目整合开发状态: Phase III
项目研究机构: Asta Medica (Originator), Degussa (Licensee)
合成路线:HECNU can be prepared as follows (2): The reaction of 2-chloroethylisocyanate (I) with activated sodium azide yields 2-chloroethylcarbamoylazide (II).The preparation of N-(2-chloroethyl)-N-nitrosocarbamoylazide (III) was performed by adding 2-chloroethylcarbamoyiazide (III) to a suspension of anhydrous sodium acetate and nitrogen tetroxide in carbon tetrachloride.Reaction of N-(2-chloroethyl)-N-nitrosocarbamoylazide (III) with ethanolamine (IV) in isopropanol yields elmustine.The described synthetic approach offers a useful means to get the nitroso group attached to the required position.
📌 参考资料/链接:
参考文献标题:Elmustine
文献作者:Castar,J.; Serradell,M.N.
参考来源:Drugs Fut 1984,9(1),18
📄 详细内容
合成路线:HECNU can be prepared as follows (2): The reaction of 2-chloroethylisocyanate (I) with activated sodium azide yields 2-chloroethylcarbamoylazide (II).The preparation of N-(2-chloroethyl)-N-nitrosocarbamoylazide (III) was performed by adding 2-chloroethylcarbamoyiazide (III) to a suspension of anhydrous sodium acetate and nitrogen tetroxide in carbon tetrachloride.Reaction of N-(2-chloroethyl)-N-nitrosocarbamoylazide (III) with ethanolamine (IV) in isopropanol yields elmustine.The described synthetic approach offers a useful means to get the nitroso group attached to the required position.
参考文献标题:Quantitative structure activity relationships of antineoplastic drugs: Nitrosoureas and triazenoimidazoles
文献作者:Hansch,C.; et al.
参考来源:Cancer Chemother Rep 1972,56443
合成路线:HECNU can be prepared as follows (2): The reaction of 2-chloroethylisocyanate (I) with activated sodium azide yields 2-chloroethylcarbamoylazide (II).The preparation of N-(2-chloroethyl)-N-nitrosocarbamoylazide (III) was performed by adding 2-chloroethylcarbamoyiazide (III) to a suspension of anhydrous sodium acetate and nitrogen tetroxide in carbon tetrachloride.Reaction of N-(2-chloroethyl)-N-nitrosocarbamoylazide (III) with ethanolamine (IV) in isopropanol yields elmustine.The described synthetic approach offers a useful means to get the nitroso group attached to the required position.
参考文献标题:Some new congeners of the anticancer 1,2-bis(2-chloroethyl)-1-nitrosourea (BCNU).Synthesis of bifunctional analogs and water soluble derivatives and preliminary evaluation of their chemotherapeutic potential
文献作者:Eisenbrand,G.; et al.
参考来源:Z Krebsforsch 1976,86279
产品链接: CAS No. 60784-46-5››