安吖啶的合成

Synthesis of Amsacrine

9-氯吖啶与2-甲氧基-4-硝基苯胺发生芳香亲核取代反应制得3-甲氧基-4-(9-吖啶基氨基)硝基苯,然后经氯化亚锡还原得3-甲氧基-4-(9-吖啶基氨基)苯胺,最后经甲磺酰化反应得到抗肿瘤药安吖啶,总收率为39%。

Amsacrine, an antitumor drug, was prepared from 9-chloroacridine via nucleophilic aromatic substitution with 2-methoxy-4-nitroaniline to give 3-methoxy-4- （9-acridinylamino） nitrobenzene, which was subjected to reduction with stannous chloride to obtain 3-methoxy-4- （9-acridinylamino） aniline, followed by methanesulfonyl reaction with an overall yield of 39 %.