Docetaxel conjugate preparation method based on mesoporous material self-assembly system

Abstract

The invention provides a method for preparing a docetaxel conjugate under a carboxyl-modified mesoporous silica self-assembly system. The method comprises the following steps: preparing carboxyl-modified mesoporous silica particles; preparing a docetaxel ester-mesoporous silica self-assembly body; in the presence of a catalyst PyBOP and a reaction assistant n-propyl phosphoric anhydride, adding acondensating agent, enabling the prepared docetaxel ester-mesoporous silica self-assembly body and a coupling component to perform an esterification reaction in a dimethylsulfoxide solvent, and generating the docetaxel conjugate. The method is capable of, through using the combination of the modification mesoporous material and a catalyst / promoter system, forming a reaction interface on the surface of the mesoporous material, promoting a coupled reaction to be performed, and greatly improving the reaction efficiency.

Description

technical field

[0001] The invention relates to a method for synthesizing a pharmaceutical compound, in particular to a method for synthesizing a docetaxel conjugate, and belongs to the fields of organic synthesis and pharmaceutical chemical synthesis. Background technique

[0002] Taxol (Paclitaxel, trade name Taxol), is a taxane diterpenoid compound isolated from Taxus (Taxus) plants. One of the good anticancer drugs. After the United States, paclitaxel as a first-line anticancer drug has been approved for marketing in more than 40 countries.

[0003] Docetaxel (Docetaxel, trade name Taxotere), chemical name 5β,20-epoxy-1,2α,4,7β,10β,13α-hexahydroxytaxane-11-en-9-one-4,10- Diacetate-2-benzoate-13-[(2'R,3'S)-N-benzoyl-3-phenylisoserine ester is a chemically modified derivative of paclitaxel, and its mechanism of action is similar to that of Paclitaxel is similar in that it promotes tubulin polymerization, inhibits microtubule depolymerization, and inhibits cell division,...