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Synthesis method of dinaverine hydrochloride

A technology of dinaverine and its synthetic method, applied in chemical instruments and methods, preparation of carboxylate, preparation of organic compounds, etc.

Active Publication Date: 2021-07-02
NINGBO SANSHENG BIOLOGICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In view of the fact that Dinavirine Hydrochloride has a great effect on the delivery of female animals, but no domestic manufacturer has obtained an approval number, and there are few patent documents reporting the synthesis method of Dinavirine Hydrochloride, the inventor independently developed a highly efficient synthetic hydrochloric acid The method of dinaverine hydrochloride, in order to realize the wide application of dinaverine hydrochloride, break the monopoly position of foreign dinaverine hydrochloride medicine

Method used

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  • Synthesis method of dinaverine hydrochloride
  • Synthesis method of dinaverine hydrochloride
  • Synthesis method of dinaverine hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Dinavirine hydrochloride of the present embodiment is obtained by following synthetic method:

[0028] S1. Add 2.86kg of acetonitrile and 4.10kg of 2,2-diphenyl-2-hydroxyacetic acid into a dry and clean reaction kettle, stir to dissolve, add 1.57kg of acetyl chloride, after the addition, stir and react at 25°C for 20 hours . After the reaction was completed, concentrate under reduced pressure until no solvent was evaporated, suck in 13.60 kg of toluene, add 1.80 kg of potassium carbonate, stir for 40 min, add 2.00 kg of anhydrous sodium sulfate and stir for dehydration, collect the filtrate by filtration, and wash the filter cake with 3.00 kg of toluene. and collect the wash solution. Combine the filtrate and the washing liquid, add 10.42 kg of potassium carbonate, and add 1.90 kg of 2-ethylbutanol. After the addition is completed, the temperature is raised to 100° C., and the reaction is stirred for 20 hours. After the reaction is complete, cool down to room temperat...

Embodiment 2

[0032] Dinavirine hydrochloride of the present embodiment is obtained by following synthetic method:

[0033] S1. Add 2.92kg of dichloromethane and 4.10kg of 2,2-diphenyl-2-hydroxyacetic acid into a dry and clean reaction kettle, stir to dissolve, add 1.89kg of propionyl chloride, and stir at 30°C to react 19.5 hours. After the reaction was completed, concentrate under reduced pressure until no solvent was evaporated, suck in 13.70 kg of toluene, add 1.52 kg of sodium carbonate, stir for 45 min, add 1.8 kg of anhydrous magnesium sulfate and stir for dehydration, collect the filtrate by filtration, and wash the filter cake with 2.85 kg of toluene. and collect the wash solution. Combine the filtrate and washing liquid, add 10.25 kg of sodium carbonate, and add 1.95 kg of 2-ethylbutanol. After the addition is completed, the temperature is raised to 105° C., and the reaction is stirred for 19.5 hours. After the reaction is complete, cool down to room temperature, filter, add 19....

Embodiment 3

[0036] Dinavirine hydrochloride of the present embodiment is obtained by following synthetic method:

[0037] S1. Add 2.45kg of chloroform and 4.10kg of 2,2-diphenyl-2-hydroxyacetic acid into a dry and clean reaction kettle, stir to dissolve, add 1.98kg of butyryl chloride, after the addition, stir and react at 20°C for 21 hours . After the reaction is complete, concentrate under reduced pressure until no solvent is evaporated, draw in 13.50 kg of toluene, add 1.25 kg of magnesium carbonate, stir for 35 minutes, add 1.65 kg of anhydrous calcium chloride and stir for dehydration, collect the filtrate by filtration, and wash the filter cake with 3.20 kg of toluene , and collect the wash solution. Combine the filtrate and the washing liquid, add 10.28 kg of magnesium carbonate, and add 1.92 kg of 2-ethylbutanol. After the addition is completed, the temperature is raised to 95° C., and the reaction is stirred for 21 hours. After the reaction is complete, cool down to room temper...

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Abstract

The invention provides a synthesis method of dinaverine hydrochloride. The method comprises the following steps: S1, reacting 2, 2-diphenyl-2-glycolic acid with acyl chloride, and then adding 2-ethyl butanol and alkali for reaction to obtain an intermediate 2-(2-ethyl butoxy)-2, 2-diphenylacetic acid; s2, adding alkali and N, N-dimethylaminochloroethane hydrochloride into the intermediate for a reaction, then introducing hydrogen chloride gas for a period of time, carrying out concentration, adding ethyl acetate, filtering, and obtaining denaverine hydrochloride.

Description

technical field [0001] The invention belongs to the technical field of chemical synthesis, and relates to a method for efficiently synthesizing dinaverine hydrochloride. Background technique [0002] Denaverine hydrochloride (Denaverine hydrochloride) is a kind of artificially synthesized derivatives of benzidine glycolic acid, and the molecular formula of the substance is (C 24 h 33 NO 3 ) HCl, the molecular weight is 420. Has the following structural formula: [0003] [0004] It is a drug that specifically reduces the contractile tension of smooth muscle tissue, and has a regulating and relaxing effect on the uterus preparing for delivery, which can enhance the sensitivity of the soft birth canal. Facilitates labor by strengthening labor contractions while supporting the elasticity of the cervix, vulva and vulva, thereby reducing the risk of maternal and fetal mortality. The drug has been launched in Spain, the Czech Republic, Bulgaria, Germany and other European ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C213/02C07C219/10
CPCC07C51/363C07C51/347C07C213/02C07C59/40C07C59/64C07C219/10
Inventor 张浩刘振强郑兴昌
Owner NINGBO SANSHENG BIOLOGICAL TECH CO LTD
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