【药物名称】Cystemustine, CMSO2EN2
化学结构式(Chemical Structure):
参考文献No.3094
标题:Novel nitrosourea cpds. Process of preparation. Compsns. based on these cpds. useful in anticancer chemotherapy
作者:Godeneche, D.; Imbach, J.-L.; Madelmont, J.-C.; Meyniel, G.; Moreau, M.-F.; Oiry, J.; Parry, D. (CNRS (Centre National de la Recherche Scientifique); INSERM (Institut National de la Sante et de la Recherche Medicale))
来源:EP 0185020; FR 2562890; JP 1988502269; WO 8504655
合成路线图解说明:

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No.22464
标题:Nitrosoureas compounds, preparation thereof and utilization thereof in anticancerous
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))
来源:US 5001158
合成路线图解说明:

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No.206732
标题:New cysteamin(2-chloroethyl)nitrosoureas. Synthesis and preliminary antitumor results
作者:Madelmont, J.C.; Godeneche, D.; Parry, D.; Duprat, J.; Chabard, J.L.; Plagne, R.; Mathe, G.; Meyniel, G.
来源:J Med Chem 1985,28(9),1346-50
合成路线图解说明:

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No.234298
标题:Cystemustine
作者:Madelmont, J.C.
来源:Drugs Fut 1994,19(1),27
合成路线图解说明:

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.

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