Duloxetine derivative and preparation thereof

Abstract

The invention relates to a duloxetine derivative and a method for preparing the same, which belongs to the chemistry field of medicine with antidepressant activity. The structural formula is as shown in the right formula, wherein R is aryl radical or tertiary butyl. The method for preparing the duloxetine derivative comprises the following steps: step one, dissolving duloxetine in dichloromethane in a reactor, adding an acid-binding agent into the mixture, stirring the mixture at room temperature for 20 minutes, and then dripping chloroacetic chloride into the mixture to react at a temperature of between 0 and 30 DEG C for 1 to 5 hours to generate an amide compound 1; and step two, dissolving the amide compound 1 generated in the step one in acetonitrile in the reactor, adding sodium iodide and triethylamine into the mixture of which the mol ratio of the amide compound 1 to the odium iodide to the triethylamine is 1 to 0.003 to (1.5 to 3), and then adding a piperazine compound into the mixture of which the mol ratio of the amide compound 1 to the piperazine compound is 1 to 1 to react at a temperature of 80 DEG C for 4 to 10 hours so as to obtain the target product. The duloxetine derivative prepared by the method has multiple mechanisms of action simultaneously, and can be used for preparing antidepressant drugs. Besides, the preparation process is simple and easy to operate.

Description

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AI Technical Summary

Benefits of technology

This new product has several actions that work together like it's making an anti-depression drug with fewer side effectings than existing products or without them altogether. It makes this way easier to use because there aren’t any extra steps needed beforehand.

Problems solved by technology

This patents discusses various methods for developing effective treatments against anxiety related diseases like major depressed patients who suffer from severe stressors due to lacking quicker acting medications without causing delays during treatment periods. Current therapies often cause unwanted side effects including sedatives and other negative aspects associated therewith. There exists a challenge towards discovering small but safe yet fast-acting agents able to provide faster and longer lastings than current ones while also reducing dosage issues over time.

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