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    • 6. 发明公开
    • 2-아미노-2-[2-[4-(3-벤질옥시페닐티오)-2-클로로페닐]에틸]-1,3-프로판디올 염산염 또는 그 수화물의 제조방법 및 그 제조 중간체
    • 制备2-氨基-2- [2- [4-(3-苄氧基]戊基] -2-氯苯基]乙基] -1,3-丙二醇氢氯化物或其水合物的方法及其中间体
    • KR1020070073895A
    • 2007-07-10
    • KR1020077010572
    • 2005-10-07
    • 교린 세이야꾸 가부시키 가이샤
    • 츠부키타케시코바야시켄이치코마츠히데타카
    • C07C319/12C07C323/07C07C323/32C07C323/56
    • C07C319/20C07C323/07C07C323/32C07C323/56
    • [PROBLEMS] To provide a process for industrially producing 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-ethyl]-1,3-propanediol hydrochloride (compound (I)), which is a compound having excellent immunosuppressive activity. [MEANS FOR SOLVING PROBLEMS] The process, which is for producing 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-ethyl]-1,3-propanediol hydrochloride, is characterized by reacting 4-(3-benzyloxyphenylthio)-2-chlorobenzaldehyde with ethyl diethylphosphonoacetate in a solvent in the presence of a base to obtain ethyl 3-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]acrylate, reducing the ethyl 3-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]acrylate, subjecting the reduced compound to mesylation, iodination, and nitration to yield 1-benzyloxy-3-[3-chloro-4-(3-nitropropyl)phenylthio]benzene, converting it to 2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-2-nitro-1,3-propanediol with formaldehyde, and then reducing it.
    • [问题]提供工业生产2-氨基-2- [2- [4-(3-苄氧基苯硫基)-2-氯苯基] - 乙基] -1,3-丙二醇盐酸盐(化合物(I))的方法,其中 是具有优异的免疫抑制活性的化合物。 解决问题的手段用于制备2-氨基-2- [2- [4-(3-苄氧基苯硫基)-2-氯苯基] - 乙基] -1,3-丙二醇盐酸盐的方法的特征在于使 4-(3-苄氧基苯硫基)-2-氯苯甲醛与二乙基膦酰基乙酸乙酯在溶剂中在碱存在下反应,得到3- [4-(3-苄氧基苯硫基)-2-氯苯基]丙烯酸乙酯,将3- [4 - (3-苄氧基苯硫基)-2-氯苯基]丙烯酸酯,将还原的化合物进行甲磺酰化,碘化和硝化,得到1-苄氧基-3- [3-氯-4-(3-硝基丙基)苯硫基]苯,将其转化 向2- [2- [4-(3-苄氧基苯硫基)-2-氯苯基]乙基] -2-硝基-1,3-丙二醇与甲醛反应,然后还原。