【药物名称】Elmustine, NSC-29485, HECNU
化学结构式(Chemical Structure):
参考文献No.154659
标题:Elmustine
作者:Casta馿r, J.; Serradell, M.N.
来源:Drugs Fut 1984,9(1),18
合成路线图解说明:

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No.800064
标题:Quantitative structure activity relationships of antineoplastic drugs: Nitrosoureas and triazenoimidazoles
作者:Hansch, C.; et al.
来源:Cancer Chemother Rep 1972,56443
合成路线图解说明:

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No.800065
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
作者:Eisenbrand, G.; et al.
来源:Z Krebsforsch 1976,86279
合成路线图解说明:

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.

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