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Synthetic method for cabazitaxel

A technology of cabazitaxel and synthetic methods, applied in the production of bulk chemicals, organic chemistry, etc., can solve the problems of reduced yield of target products, increased process costs, complicated purification steps, etc., achieves mild hydrolysis reaction conditions and shortens the reaction cycle , the effect of improving yield and purity

Inactive Publication Date: 2012-09-19
CHONGQING BEISHENG PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

C 7 and C 10 The hydroxyl group can be methylated, C 13 The hydroxyl group is also exposed and easily methylated, resulting in many by-products and a decrease in the yield of the target product, and the subsequent purification steps are complicated, resulting in an increase in process costs

Method used

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Embodiment 2

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Abstract

The invention discloses a synthetic method for cabazitaxel, and the synthetic method comprises the following steps: performing double methylation on the C7 site and C10 site of a compound A so as to obtain a compound B, and hydrolyzing the comound B under the acidity condition so as to obtain the cabazitaxel. The cabazitaxel has a reaction formula shown in the specification. Compared with the prior art, the synthetic method has the advantage that the compound A of which the C13-site hydroxyl is connected with a protecting group is used as a raw material, and a method of obtaining the cabazitaxel by virtue of double methylation of the C7-site and C10-site hydroxyl and hydrolysis, so that a step of generating by-products by the methylation of the C13-site hydroxyl of 10-Deacetylbaccatin III and a complex purification step are omitted. The synthetic method has the advantages of simple technology and moderate reaction condition, and can be used for improving the yield and purity of the cabazitaxel.

Description

technical field The invention relates to the field of drug synthesis, in particular to a synthesis method of cabazitaxel. Background technique Cabazitaxel (English name Cabazitaxel, trade name Jevtana) is a taxane compound, molecular formula C 45 h 57 NO 14 , with a molecular weight of 835.93, is similar in structure to the anticancer drugs paclitaxel and docetaxel. On June 17, 2010, the U.S. Food and Drug Administration (FDA) approved cabazitaxel as a second-line therapy for the treatment of prostate cancer. The drug is used in combination with prednisone to treat patients with metastatic hormone-refractory prostate cancer (mHRPC) who have previously been treated with a docetaxel-containing regimen. The anti-cancer mechanism and characteristics of Cabazitaxel are similar to those of docetaxel, and it belongs to anti-microtubule drugs. Cabazitaxel binds to tubulin, promotes its assembly into microtubules, and at the same time prevents the disassembly of these assembled...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D305/14
CPCY02P20/55
Inventor 白金生陈大海陈从均
Owner CHONGQING BEISHENG PHARMA TECH CO LTD
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