【摘要】 对妥曲珠利(1)的合成工艺进行了改进。4-三氟甲硫基苯酚和2-甲基-4-硝基氯苯通过芳香亲核取代、催化氢化反应后,用安全、无污染的固体光气代替原来剧毒的光气与得到的3-甲基-4-(4-三氟甲硫基苯氧基)-苯胺(3)进行光气化反应,制得3-甲基-4-(4-三氟甲硫基苯氧基)-苯基异氰酸酯(4)。化合物4与甲基脲反应得到异构的缩二脲衍生物(5和6),无需分离,在甲醇钠催化下与碳酸二甲酯环合,制得目标产物,总收率71%。更多还原

【Abstract】 An improved process for preparing toltrazuril(1) was described.The important intermediate phenylamino derivative(3) was prepared from 4-[(trifluoromethyl)thio]-phenol and 1-chloro-2-methyl-4-nitro-benzene by aromatic nucleophilic substitution and catalytic hydrogenation,then was phosgenated by using BTC instead of phosgene.The isomeric biurets(5 and 6) were prepared by the reaction of phenylisocyanate(4) with methylurea.Finally,1 was prepared by the reaction of 5 and 6 with dimethyl carbonate and sodium methoxide with an overall yield of 71%.更多还原