合成路线:The reaction of 4-nitrophenol (I) with 2-chloroethyl isocyanate (II) in pyridine leads to the activated carbamate (III),which is nitrosated by reacting with nitrosyl chloride in pyridine at -20 C to yield 4-nitrophenyl N-(2-chloroethyl)-N-nitrosocarbamate (IV).The nitrosated molecule (IV) is reacted with 2-(methylthio)ethylamine (V) in THF at ordinary temperature affording the sulfure urea (VI),which is then oxidized to the sulfonyl compound (VII) by hydrogen peroxide in formic acid at 50 C.
参考文献标题:Nitrosoureas compounds,preparation thereof and utilization thereof in anticancerous
文献作者:Madelmont,J.-C.; Godeneche,D.; Moreau,M.-F.; Parry,D.; Meyniel,G.; Oiry,J.; Imbach,J.-L.(CNRS (Centre National de la Recherche Scientifique); INSERM (Institut National de la Sante et de la Recherche Medicale))
参考来源:US 5001158
合成路线:The reaction of 4-nitrophenol (I) with 2-chloroethyl isocyanate (II) in pyridine leads to the activated carbamate (III),which is nitrosated by reacting with nitrosyl chloride in pyridine at -20 C to yield 4-nitrophenyl N-(2-chloroethyl)-N-nitrosocarbamate (IV).The nitrosated molecule (IV) is reacted with 2-(methylthio)ethylamine (V) in THF at ordinary temperature affording the sulfure urea (VI),which is then oxidized to the sulfonyl compound (VII) by hydrogen peroxide in formic acid at 50 C.
参考文献标题:New cysteamin(2-chloroethyl)nitrosoureas.Synthesis and preliminary antitumor results
文献作者:Madelmont,J.C.; Godeneche,D.; Parry,D.; Duprat,J.; Chabard,J.L.; Plagne,R.; Mathe,G.; Meyniel,G.
参考来源:J Med Chem 1985,28(9),1346-50
合成路线:The reaction of 4-nitrophenol (I) with 2-chloroethyl isocyanate (II) in pyridine leads to the activated carbamate (III),which is nitrosated by reacting with nitrosyl chloride in pyridine at -20 C to yield 4-nitrophenyl N-(2-chloroethyl)-N-nitrosocarbamate (IV).The nitrosated molecule (IV) is reacted with 2-(methylthio)ethylamine (V) in THF at ordinary temperature affording the sulfure urea (VI),which is then oxidized to the sulfonyl compound (VII) by hydrogen peroxide in formic acid at 50 C.
参考文献标题:Cystemustine
文献作者:Madelmont,J.C.
参考来源:Drugs Fut 1994,19(1),27
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