Tauromustine, TCNU, LS-2667, Tauricyt

牛磺莫司汀Chemical Name: 1-(2-Chloroethyl)-3-[2-(dimethylsulfamoyl)ethyl]-1-nitrosurea
CAS No. 85977-49-7
项目整合开发状态: Phase III
项目研究机构: Leo (Originator)
合成路线: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:2) By condensation of (I) with N-(2-chloroethyl)-N-nitrosocarbamoyl hydrazide (IV) in ethanol with triethylamine as catalyst.

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