Tauromustine, TCNU, LS-2667, Tauricyt-药物合成数据库

【药物名称】Tauromustine, TCNU, LS-2667, Tauricyt

化学结构式(Chemical Structure):

参考文献No.	41904
标题:	N-nitroso compounds and compositions containing such compounds
作者:	Carlsson, J.-I.; Jensen, P.H.G.; Stamvik, A.R. (Leo Pharma AB)
来源:	EP 0106123; JP 59073562; US 4613695

合成路线图解说明: 1) N,N-Dimethyl-2-aminoethanesulfonamide (I) is condensed with 2-chloroethyl isocyanate (II) by means of triethylamine in CHCl3 giving 1-(2-chloroethyl)- isocyanate (II) by means of triethylamine in CHCl3 giving 1-(2-chloroethyl)-3-[2-(dimethylsulfamoyl)ethyl]urea (III), which is nitrosated with NaNO3, N2O4 or NOCl in acetic acid-acetic anhydride.

合成路线图解说明: 2) By condensation of (I) with N-(2-chloroethyl)-N-nitrosocarbamoyl hydrazide (IV) in ethanol with triethylamine as catalyst.

合成路线图解说明: 3) By condensation of (I) with 1-[N-(2-chloroethyl)-N-nitrosocarbamoyloxy]pyrrolidine-2,5-dione (V) in methanol with triethylamine as catalyst.

合成路线图解说明: 4) By condensation of (I) with 4-nitrophenyl N-(2-chloroethyl)-N-nitrosocarbamate (VI) in methanol with triethylamine as before.

参考文献No.	51512
标题:	Tauromustine
作者:	Prous, J.; Casta馿r, J.
来源:	Drugs Fut 1986,11(7),585

合成路线图解说明: 1) N,N-Dimethyl-2-aminoethanesulfonamide (I) is condensed with 2-chloroethyl isocyanate (II) by means of triethylamine in CHCl3 giving 1-(2-chloroethyl)- isocyanate (II) by means of triethylamine in CHCl3 giving 1-(2-chloroethyl)-3-[2-(dimethylsulfamoyl)ethyl]urea (III), which is nitrosated with NaNO3, N2O4 or NOCl in acetic acid-acetic anhydride.

合成路线图解说明: 2) By condensation of (I) with N-(2-chloroethyl)-N-nitrosocarbamoyl hydrazide (IV) in ethanol with triethylamine as catalyst.

合成路线图解说明: 3) By condensation of (I) with 1-[N-(2-chloroethyl)-N-nitrosocarbamoyloxy]pyrrolidine-2,5-dione (V) in methanol with triethylamine as catalyst.

合成路线图解说明: 4) By condensation of (I) with 4-nitrophenyl N-(2-chloroethyl)-N-nitrosocarbamate (VI) in methanol with triethylamine as before.