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[洋红霉素和柔红霉素的新衍生物]

[New derivatives of carminomycin and rubomycin].

作者信息

Olsuf'eva E N, Aleksandrova L G, Rozynov B V, Potapova N P

出版信息

Antibiot Khimioter. 1988 Oct;33(10):729-35.

PMID:3214206
Abstract

For preparing new semisynthetic analogs of anthracycline antibiotics, hydrolysis of 13-dimethylketals of 14-bromrubomycin and 14-brom-arminomycin in solution of diluted hydrochloric acid was studied. It was shown that such hydrolysis yielded 14-chlorrubomycin and 14-chlorcarminomycin. Conditions for separating the mixture of 14-chlor- and 14-bromrubomycins and the mixture of 14-chlor- and 14-bromcarminomycins by HPLC were developed. Interaction of 14-chlorine derivatives of rubomycin and carminomycin with potassium formate in the presence of the crown ether yielded 14-formyloxy derivatives of rubomycin and carminomycin. Interaction of rubomycin and carminomycin with formic acid in the presence of N-oxysuccinimide and dicyclohexylcarbodiimide resulted in formation of N-formyl derivatives of rubomycin and carminomycin.

摘要

为制备蒽环类抗生素的新型半合成类似物,研究了14-溴柔红霉素和14-溴阿霉素的13-二甲基缩酮在稀盐酸溶液中的水解反应。结果表明,这种水解反应生成了14-氯柔红霉素和14-氯洋红霉素。开发了通过高效液相色谱法分离14-氯柔红霉素和14-溴柔红霉素混合物以及14-氯洋红霉素和14-溴洋红霉素混合物的条件。柔红霉素和洋红霉素的14-氯衍生物在冠醚存在下与甲酸钾相互作用,生成了柔红霉素和洋红霉素的14-甲酰氧基衍生物。柔红霉素和洋红霉素在N-氧代琥珀酰亚胺和二环己基碳二亚胺存在下与甲酸相互作用,生成了柔红霉素和洋红霉素的N-甲酰基衍生物。

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