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Synthesis of chlorambucil-dopamine conjugate and preparation of prodrug nanoparticles of chlorambucil-dopamine conjugate

A technology of chlorambucil and nanoparticles, applied in the field of chemical industry, can solve problems such as single chemotherapy system, difficult transformation and application, no synergistic performance research of chemotherapy and photothermal therapy, etc., achieve mild reaction conditions, easy operation, design reasonable effect

Active Publication Date: 2018-08-10
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Moreover, the therapeutic research of self-assembled vesicles mentioned above is limited to a single chemotherapy system, and there is no synergistic research on the integration of chemotherapy and photothermal therapy, which is difficult to transform and apply in the clinic

Method used

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  • Synthesis of chlorambucil-dopamine conjugate and preparation of prodrug nanoparticles of chlorambucil-dopamine conjugate
  • Synthesis of chlorambucil-dopamine conjugate and preparation of prodrug nanoparticles of chlorambucil-dopamine conjugate
  • Synthesis of chlorambucil-dopamine conjugate and preparation of prodrug nanoparticles of chlorambucil-dopamine conjugate

Examples

Experimental program
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Effect test

Embodiment 1

[0053] Step 1: Dissolve 1000mg of 3,4-dihydroxyphenylpropionic acid in 20mL of anhydrous acetone, slowly drop 383μL of phosphorus trichloride into the above reaction flask, and react in an ice-water bath at 0°C for 6 After hours, the water pump rotavaps. The crude product was dissolved in a mixture of water and ether, extracted with a separatory funnel, the organic layer was extracted three times with water, concentrated and dried to obtain white powder 2,2-dimethyl-1,3-benzodioxolane ene-5-propionic acid. Yield 60%.

[0054] Step 2, 222mg of 2,2-dimethyl-1,3-benzodioxol-5-propionic acid, 247.2mg of dicyclohexylcarbodiimide, 146.4mg of 4-dimethylamino Pyridine was dissolved in 5 mL of anhydrous dichloromethane. After reacting at room temperature for 4 hours, 180 mg of 2-hydroxyethyl disulfide in dichloromethane was dropped dropwise into the reaction flask. After reacting at room temperature for 48 hours, it was rotovaped. The column was packed with dichloromethane, and the...

Embodiment 2

[0061] The steps of this example are the same as those of Example 1, except that in Step 4, the masses of dopamine hydrochloride and chlorambucil-dopamine conjugate molecules are 12.5 mg and 17.4 mg, respectively. The yield of this embodiment is 30%~40%.

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Abstract

The invention relates to a method for preparing a chlorambucil-dopamine conjugate and prodrug nanoparticles of the chlorambucil-dopamine conjugate. The method comprises the steps of: synthesizing 2,2-dimethyl-1,3-benzodioxole-5-propionic acid, then synthesizing 2-(2-hydroxyethyl)dithioxo)ethyl-2,2-dimethyl-1,3-benzodioxole-5-ethyl propionate, then synthesizing ((2-(2,2-dimethyl-1,3-benzodioxole)-5-propionyl)oxy)ethyl)-4-(4-(bis(2-chloroethyl)amino)phenyl)methyl butyrate, then synthesizing the chlorambucil-dopamine conjugate, and finally synthesizing the prodrug nanoparticles of the chlorambucil-dopamine conjugate. A simple and effective route is provided for preparation of the chlorambucil-dopamine conjugate and the prodrug nanoparticles of the chlorambucil-dopamine conjugate, and an experimental platform is provided for acquisition of a polymer drug carrier which has near-infrared light absorption, reduction response and integrated photothermal therapy and chemotherapy.

Description

technical field [0001] The invention relates to the technical field of chemical industry, in particular to the synthesis of a chlorambucil-dopamine conjugate and the preparation method of chlorambucil-polydopamine prodrug nanoparticles. Background technique [0002] A new generation of polymeric prodrug nanoparticles with multiple stimuli responsiveness and good biocompatibility has broad applications in the field of cancer therapy. The release behavior of anticancer drugs can be regulated by stimuli such as pH value, temperature, redox, and light. At the same time, polymer-drug conjugate nanoparticles can be enriched in tumor tissues through targeting, reducing the side effects of chemotherapy drugs on healthy tissues. Improve the efficacy of chemotherapy. On the other hand, photothermal therapy is a low-invasive, high-efficacy cancer treatment method, and the effect of cancer treatment can be further improved by combining photothermal therapy with chemotherapy drugs. For...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C319/22C07C323/12A61K31/196A61K41/00A61K47/55A61K47/59A61P35/00C08G73/06
CPCA61K31/196A61K41/0052A61K47/55A61K47/59A61P35/00C07C319/22C07D317/46C08G73/0672C07C323/12
Inventor 杜畅董常明张蓉
Owner SHANGHAI JIAO TONG UNIV
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