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A new type of taxane compound, its production method and application

机译:一种新型紫杉烷类化合物及其生产方法和应用

摘要

The present invention discloses a new type of taxane compound and its preparation and application. A method for producing a new type of taxane compound comprises the following steps: protecting two hydroxyl groups in gemcitabine, carrying out a condensation reaction between protected gemcitabine and alkyl chloroformate, removing the hydroxyl protecting group and intermediates Obtaining G1, protecting the primary hydroxyl group of intermediate G1, then protecting the other one of the hydroxyl groups and removing the protecting group of the primary hydroxyl group to obtain intermediate G2, 7, Reacting 10-di-troc-docetaxel with dianhydride to obtain intermediate D1, performing a condensation reaction between intermediate D1 and intermediate G2 to obtain intermediate D2, and intermediate A step of subjecting D2 to hydroxyl deprotection to obtain a target compound. The new types of taxane compounds of the present invention have low toxicity and high anti-tumor activity and have good inhibition rates, especially against solid tumors such as leukemia and gastrointestinal cancer, lung cancer and breast cancer.
机译:本发明公开了一种新型的紫杉烷类化合物及其制备和应用。一种新型紫杉烷类化合物的制备方法包括以下步骤:保护吉西他滨中的两个羟基;在被保护的吉西他滨与氯甲酸烷基酯之间进行缩合反应;除去羟基保护基团和中间体;获得G1;保护甲壳素的伯羟基。中间体G1,然后保护另一个羟基并除去伯羟基的保护基,得到中间体G2,7,使10-二-troc-多西他赛与二酐反应得到中间体D1,在中间体之间进行缩合反应D1和中间体G2获得中间体D2,以及中间体A使D2进行羟基脱保护以获得目标化合物的步骤。本发明的新型紫杉烷化合物具有低毒性和高抗肿瘤活性,并且具有良好的抑制率,尤其是针对实体瘤如白血病和胃肠道癌,肺癌和乳腺癌。

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