Water-soluble paclitaxel ester compounds containing 1,2,3-triazole and preparation method

A technology for paclitaxel esters and compounds, which is applied in the directions of medical preparations containing active ingredients, organic chemistry, pharmaceutical combinations, etc., can solve the problems of complicated separation, easy precipitation, and reduced product yield, and achieves simplified synthesis steps and increased water solubility. , the effect of easy availability of raw materials
CN101391995AActive Publication Date: 2009-03-25SHANGHAI TIANCI INT PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHANGHAI TIANCI INT PHARMA
Publication Date
2009-03-25

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Abstract

The invention relates to a water-soluble paclitaxel ester containing 1, 2, 3-triazole, and a preparation method thereof, which takes paclitaxel as the raw material to carry out esterification reaction with 4-alkynyl benzoic acid under the existence of the dehydrating agent, dicyclohexylcarbodiimide (DCC) and 4-dimethylamino pyridine (DMAP), so as to synthetize the paclitaxel molecule containing alkynyl, and then carries out 1, 3-dipolar cycloaddition reaction with water-soluble azido-acetic acid or 4-azido-benzoic acid under the existence of the catalyst, Cu(I), and sodium ascorbate, thus quickly, simply and conveniently synthetizing the water-soluble paclitaxel containing carboxylic group. Compared with the existing paclitaxel, the water-soluble paclitaxel which is synthetized by the invention and contains water-soluble carboxylic group and polarity 1, 2, 3-triazole heterocycle improves the water-solubility and can be used for curing various cancers. The invention has the advantages of mild reaction condition in the method for preparing the water-soluble paclitaxel, easy post treatment, high yield and being suitable for industrial production.
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Description

technical field

[0001] The invention relates to a water-soluble taxol ester compound containing 1,2,3-triazole and a preparation method thereof. The compound can be used for treating various cancers. Background technique

[0002] Paclitaxel is a natural organic compound extracted from yew leaves, bark, branches and other parts. It has broad-spectrum anti-cancer properties and has a strong killing effect on tumor cells such as uterine cancer, breast cancer, lung cancer and leukemia. [1] . Due to the special curative effect of paclitaxel, it is listed as the first choice anti-cancer drug by the United States and other developed countries. According to the statistics of the United States in 2006, the total sales of paclitaxel preparations in the international market, including paclitaxel injections processed from natural raw materials and semi-synthetic paclitaxel injections, have reached 3.7 billion US dollars, ranking first in the world's anticancer drugs. Dr. Samuel Broder...

Claims

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