N，N’－双氯乙基脲和卡莫司汀的合成研究

摘要

用2－恶唑烷酮、乙醇胺和氯化亚砜制备N，N’－双氯乙基脲，再加入甲酸和亚硝酸钠制得卡莫司汀。分别考察了物料比、反应温度、反应时间等参数，得到N，N’－双氯乙基脲最佳反应条件为：于120℃搅拌加热2h，自然冷却至0℃，加过量氯化亚砜，温度控制在20℃以下。加毕后升温至100℃反应2h。稍降温后加入乙醇和活性炭回流脱色，过滤。在此条件下，N，N’－双氯乙基脲收率达34．4％。%With 2 - oxazolidinone, ethanolamine and thionyl chloride prepared N, N'- Mechlorethamine urea, and then added with formic acid and sodium nitrite was prepared carmustine. Were investigated the ratio of materials, reaction temperature, reaction time and other parameters, to obtain N, N '- Mechlorethamine urea optimum reaction conditions as follows: heated with stirring at 120 ℃ 2h, naturally cooled to 0 ℃, add excess thionyl chloride temperature control in less than 20 ℃. Heated to 100 ℃ plus complete reaction 2h. After cooling slightly, adding ethanol and reflux for decolorization of activated carbon, and filtered. Under this condition, the N, N'- Mechlorethamine urea yield of 34.4%.