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3′-脱氨基-3′-(3-氰基-4-吗啉基)阿霉素比阿霉素的活性要高得多,且在动物试验中几无心脏毒性,但合成产率很低。研究表明其抗肿瘤活性与 N-取代基的体积和电子效应有关。据此我们由不同的酸酐及其它原料通过三种方法合成了11个 N 取代的柔红
3’-deamino-3’- (3-cyano-4-morpholino) doxorubicin is much more active than doxorubicin and has few cardiotoxicity in animal tests, but the yield of synthesis is very high low. Studies have shown that its anti-tumor activity and the N-substituent volume and electronic effects. Based on this, we synthesized 11 N-substituted soft reds from different anhydrides and other raw materials through three methods