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Preparation method of ftibamzone

A technology of phthalocyanine and n-butyraldehyde, which is applied in the synthesis field of antiviral drugs, can solve the problems of complex reaction process, relatively many conditional restrictions, long reaction steps and the like, and achieves high yield, high purity and few reaction steps. Effect

Active Publication Date: 2021-02-09
山东嘉成医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Existing phthalobutanol synthesis method has complex reaction process, long reaction steps, many conditional restrictions in the reaction process, and low yield of phthalobutane obtained, etc.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] The preparation method of embodiment 1 phthalobutanol, the steps are as follows:

[0023] (1) Synthesis of 3-phthalimide-butanone: put 185 grams of phthalimide potassium salt and 500 ml of DMF into a 1000ml reaction bottle, and add 106.5 grams of 3-chlorobutanone dropwise at 20°C , after dropping, keep it warm at 25°C for 8 hours; after the reaction, add 250ml of purified water dropwise, filter, wash with water, and dry to obtain 206 grams of 3-phthalimide-butanone, with a yield of 95%;

[0024] (2) Preparation of 3-phthalimide-2-oxo-n-butyraldehyde: put 206 grams of 3-phthalimide-butanone and 6000 ml of dimethyl sulfoxide into a 1000ml reaction bottle, and control the temperature at 45°C Feed 81 grams of dry hydrogen bromide gas, control the ventilation rate to 0.4 grams per minute, and complete the heat preservation reaction for 2 hours; obtain the dimethyl sulfoxide solution of 3-phthalimide-2-oxo-n-butyraldehyde, Proceed directly to the next step without separation...

Embodiment 2

[0026] Embodiment 2 The preparation method of phthalobutanol, the steps are as follows:

[0027] (1) Synthesis of 3-phthalimide-butanone: Put 185 grams of phthalimide potassium salt and 500 ml of DMF into a 1000ml reaction bottle, and add 106.5 grams of 3-chlorobutanone dropwise at 25°C , after dropping, keep it warm at 30°C for 8 hours; after the reaction, add 250ml of purified water dropwise, filter, wash with water, and dry to obtain 208 grams of 3-phthalimide-butanone, with a yield of 96%;

[0028] (2) Preparation of 3-phthalimide-2-oxo-n-butyraldehyde: put 206 grams of 3-phthalimide-butanone and 6000 ml of dimethyl sulfoxide into a 1000ml reaction bottle, and control the temperature at 50°C Feed 81 grams of dry hydrogen bromide gas, control the ventilation rate to 0.3 grams per minute, and complete the heat preservation reaction for 2 hours; obtain the dimethyl sulfoxide solution of 3-phthalimide-2-oxo-n-butyraldehyde, Proceed directly to the next step without separation...

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Abstract

The invention discloses a preparation method of ftibamzone. The preparation method comprises the following steps: firstly, preparing 3-phthalimide butanone from phthalimide potassium salt and 3-chlorobutanone; reacting the 3-phthalimide butanone with dry hydrogen bromide gas in a dimethyl sulfoxide solution to prepare a dimethyl sulfoxide solution of 3-phthalimide-2-oxy-n-butyraldehyde; dropwise adding a thiosemicarbazide solution into the dimethyl sulfoxide solution of the 3-phthalimide-2-oxy-n-butyraldehyde, controlling the reaction temperature, carrying out heat preservation reaction to prepare a crude product, and recrystallizing the crude product to obtain the ftibamzone. The technical scheme has the advantages of few reaction steps, high yield and high purity.

Description

technical field [0001] The invention relates to a synthesis method of an antiviral drug, in particular to a preparation method of high-yield and high-purity phthalobutamol. Background technique [0002] Phthalobutanol, the chemical name is 3-phthalimide-2-oxo-n-butyraldehyde bisthiosemicarbazone V. Phthalin is a thiosemicarbazone antiviral drug. It has anti-Chlamydia trachomatis and anti-herpes virus activity, and its inhibitory effect on Chlamydia trachomatis is 10 times stronger than aureomycin, and can prevent the reproduction of Chlamydia trachomatis and the formation of inclusion bodies. Its mechanism of action is mainly to inhibit viral DNA and early protein synthesis. It is commonly used clinically for herpes zoster, herpes simplex, condyloma acuminatum, superficial fungal infection and various trachoma. [0003] The existing phthalobutanol synthesis method has problems such as complicated reaction process, long reaction steps, many condition restrictions in the re...

Claims

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Application Information

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IPC IPC(8): C07D209/48
CPCC07D209/48
Inventor 王平生赵士杰梁志红刘宏林
Owner 山东嘉成医药科技有限公司
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