Filer C N, Granchelli F E, Soloway A H, Neumeyer J L
J Med Chem. 1977 Nov;20(11):1504-8. doi: 10.1021/jm00221a030.
A series of 3-amino-4-(p-aminophenyl)isoquinolines bearing the bis(2-chloroethyl)amino group was synthesized as potential CNS antitumor agents. Diol precursors 1e and 1f were prepared by the treatment of 1b and 1c with ethylene oxide. Diol precursors 5a-c and 9 were prepared by the treatment of 4a-c and 8 with diethanolamine. The reaction of these diols with SOCl2 yielded target mustards 10-15 which were evaluated in the intraperitoneal murine L1210 tumor. No intermediates or target mustards were active in this tumor system.
合成了一系列带有双（2-氯乙基）氨基的3-氨基-4-（对氨基苯基）异喹啉作为潜在的中枢神经系统抗肿瘤剂。二醇前体1e和1f通过用环氧乙烷处理1b和1c制备。二醇前体5a-c和9通过用二乙醇胺处理4a-c和8制备。这些二醇与亚硫酰氯反应生成目标芥子气10-15，并在小鼠L1210腹腔肿瘤中进行评估。在该肿瘤系统中，没有中间体或目标芥子气具有活性。
