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根据阿霉素、DHAD及Showalter等1984年合成的吡唑并蒽醌衍生物的生物活性,以及“嵌入”DNA的作用机理,设计合成了20个A环无取代的吡唑并[3,4,5-mn]蒽醌衍生物(Ⅰ)及6个A环7,10位有二氯取代的吡唑并蒽醌衍生物(Ⅱ)。将1,4-二羟基-9,10-蒽醌二对甲苯磺酰化,其产物与单烷基肼在室温下缩合形成吡唑环,然后与胺反应
According to the biological activity of pyrazoloanthraquinone derivatives synthesized by doxorubicin, DHAD and Showalter in 1984, and the mechanism of “embedded” DNA, 20 A ring unsubstituted pyrazolo [3,4 , 5-mn] anthraquinone derivatives (Ⅰ) and six A ring 7,1,10,10-dichloro-substituted pyrazoloanthraquinone derivatives (Ⅱ). 1,4-Dihydroxy-9,10-anthraquinone di-tosylate, the product of which is condensed with a monoalkylhydrazine at room temperature to form a pyrazole ring, which is then reacted with an amine