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Synthetic method for dapoxetine

A technology for dapoxetine and a synthesis method, which is applied in the field of medicinal chemistry, can solve the problems of harsh reaction conditions, difficult procurement of raw materials, and complicated reaction steps, and achieves the effects of simplifying separation steps, simplifying reaction procedures, and reducing raw material costs.

Inactive Publication Date: 2006-08-23
上海玛耀化学技术有限公司
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AI Technical Summary

Benefits of technology

This patented technology involves making certain chemicals from 2-(halo)phenol by reducing costs while maintaining their effectiveness or improving efficiency during reactions like nitrogen fixations.

Problems solved by technology

This patents describes various technical problem addressed during research on pharmaceuticals called diabetes modifiers (DDM's). Diabetic individuals often require medications to reduce their risk factors associated with these diseases. These include high blood pressure levels caused by insulins regulating peripheral glucose metabolism, increased chances of heart attacks, stroke symptoms, renal failure, cardiac arrests/failures, pulmonary embolisms, gastrointestinal bleeding, urinary retention, etc., among others. There currently exist no specific medicine approved specifically targeting DIAMTES but there still remains an issue where current options either lack effectiveness or involve complicated procedures.

Method used

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  • Synthetic method for dapoxetine
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  • Synthetic method for dapoxetine

Examples

Experimental program
Comparison scheme
Effect test

example 27

[0023] NN-Dimethyl-1-phenyl-3-(1-naphthyloxy)propylamine oxalate, melting point 116-118°C.

[0024] Analyze and press C 23 h 25 NO 5 calculate:

[0025] Theoretical values: C 69.86, H 6.37, N 3.54

[0026] Experimental values: C 70.02, H 6.37, N 3.43

example 28

[0028] NN-Dimethyl-1-phenyl-3-(1-naphthyloxy)propylamine p-benzenesulfonate, melting point 98-110°C, decomposed.

[0029] Analysis and calculation according to C28H31NO4S:

[0030] Theoretical values: C 70.40, H 6.54, N 2.93

[0031] Experimental values: C 70.29, H 6.55, N 3.16

example 36

[0033] (+)NN-Dimethyl-1-phenyl-3-(1-naphthyloxy)propylamine tartrate

[0034] 32.44 g (0.106 mol) of NN-dimethyl-1-phenyl-3-(1-naphthyloxy)propylamine was dissolved in 75 ml of ethanol, and 15.94 g (0.106 mol) of (+)-tartaric acid was dissolved in 650 The solutions in mL of water were combined. The mixture was left at room temperature overnight and the precipitated solid was vacuum filtered. The title compound of this example was finally isolated by multiple recrystallizations, m.p. 94-96°C.

[0035] Analyze and calculate according to C25H29NO7:

[0036] Theoretical values: C 65.92, H 6.42, N 3.08

[0037] Experimental values: C 65.92, H 6.48, N 3.00

[0038] other information:

[0039]

[0040] US Patent: 5,292,962

[0041]

[0042] Although the starting materials produced in the above methods are different, the reaction conditions are harsh, the raw materials are not easy to purchase, and the reaction steps are cumbersome.

Invention content:

[0043] The techn...

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Abstract

The present invention discloses the synthesis method of dapoxetine. The method of the present invention adopts 3-chlorophenyl ethanone as initial material, has shortened reaction process, lowered cost and simple operation, and is suitable for industrial production.

Description

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Claims

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Application Information

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Owner 上海玛耀化学技术有限公司
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