Studies on Antitumor Substances. XII. Synthesis of Bis (2, 3-epoxypropyl) amine Derivatives and the Reaction with Some Nucleophiles
作者:SEIGORO HAYASHI、MITSURU FURUKAWA、YOKO FUJINO、MAKOTO SUGITA、TORU NAKAO
DOI:10.1248/cpb.19.2003
日期:——
Several bis (2, 3-epoxypropyl) amine derivatives were successfully synthesized by the modification of Homer's method. N, N'-Bis (2, 3-epoxypropyl) piperazine and p-bis (2, 3-epoxypropoxy) benzene were attempted to react with thiols, amines and phenol, and the corresponding ring opening compounds of the epoxide ring were obtained in good yields, respectively. N, N'-Bis (2, 3-epoxypropyl) piperazine and p-bis (2, 3-epoxypropoxy) benzene also reacted with diethyl malonate to give N, N'-bis (γ-ethoxycarbonyl-γ-butyrolacton-α-yl) methyl piperazine and p-bis (γ-ethoxycarbonyl-γ-butyrolacton-α-yl) methoxy benzene, respectively.
通过修改 Homer 方法,成功合成了几种双(2,3-环氧丙基)胺衍生物。尝试将 N,N'-双(2,3-环氧丙基)哌嗪和对(2,3-环氧丙氧基)苯与硫醇、胺和苯酚反应,分别以良好的收率获得了相应的环氧化物开环化合物。N,N'-双(2,3-环氧丙基)哌嗪和对(2,3-环氧丙氧基)苯也分别与丙二酸二乙酯反应,得到 N,N'-双(γ-乙氧羰基-γ-丁内酯-α-基)甲基哌嗪和对(γ-乙氧羰基-γ-丁内酯-α-基)甲氧基苯。