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Novel method for preparing high-purity propofol

A propofol, high-purity technology, applied in the field of medicine, can solve the problems of high reaction cost, high equipment requirements, difficult removal, etc., and achieves the effects of simple post-processing, low equipment cost, and low environmental protection cost.

Active Publication Date: 2012-07-25
云南龙海天然植物药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The first two methods require high temperature and high pressure conditions, and relatively high equipment requirements; while the reaction conditions of the latter method are relatively mild, but the carboxyl positioning group needs to be removed, and the reaction cost is relatively high
Moreover, in the above three methods for preparing propofol, due to the inconspicuous positioning effect of substituents, a large amount of by-products with similar structures and difficult to remove are produced in the alkylation reaction process, making it difficult to effectively obtain the relevant substance content of the drug. control; in addition, these useless phenolic by-products will cause great environmental pressure

Method used

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  • Novel method for preparing high-purity propofol
  • Novel method for preparing high-purity propofol
  • Novel method for preparing high-purity propofol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Add 1000 g (30%, 3.0 mol) of sulfuric acid into a 3 L flask, add 177 g (1.0 mol) of 2,6-diisopropylaniline under stirring, and stir to dissolve until clear. Cool to -5°C, slowly add dropwise a solution of 69g (1.0mol) sodium nitrite and 210ml of water, stir for about 20min after the addition, and store at -5°C for later use. Add 800 g of 25% sulfuric acid into the 3L flask, heat to 127°C, drop the diazonium salt solution in batches, and continue the reaction for about 2 hours. After the reaction solution was cooled, it was extracted three times with 80ml toluene, and the organic phases were combined and separated by distillation, and the 87-89°C / 2mmHg fraction was collected with a purity of >99% (GLC).

Embodiment 2

[0028] Add 910 g (10%, 2.5 mol) of hydrochloric acid into a 3 L flask, add 177 g (1.0 mol) of 2,6-diisopropylaniline under stirring, and stir to dissolve until clear. Cool to 15°C, slowly add dropwise 104g (1.5mol) of sodium nitrite and 155ml of water to obtain a solution, stir for about 20 minutes after the addition, and store at -5°C for later use. Add 500 g of 30% hydrochloric acid into a 3 L flask, heat to 105° C., drop the diazonium salt solution in batches, and continue the reaction for about 2 h. After the reaction solution was cooled, it was extracted three times with 80ml toluene, and the organic phases were combined and separated by distillation, and the 87-89°C / 2mmHg fraction was collected with a purity of >99% (GLC).

Embodiment 3

[0030] Add 245g (60%, 1.5mol) of phosphoric acid into a 3L flask, add 177g (1.0mol) of 2,6-diisopropylaniline under stirring, stir and dissolve until clear. Cool to 5°C, slowly add dropwise 55g (0.8mol) of sodium nitrite and 495ml of water to obtain a solution, stir for about 20 minutes after the addition, and store at -5°C for later use. Add 300 g of 70% phosphoric acid into a 3 L flask, heat to 120° C., drop the diazonium salt solution in batches, and continue the reaction for about 2 h. After the reaction solution was cooled, it was extracted three times with 80ml toluene, and the organic phases were combined and separated by distillation, and the 87-89°C / 2mmHg fraction was collected with a purity of >99% (GLC).

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Abstract

The invention provides a synthetic method for preparing a high-purity anesthetic, i.e., propofol (I). According to the method, the problem of difficulty in removing a large quantity of impurities with similar structures produced in the conventional preparation method is solved, and the emission of phenol pollutants is reduced.

Description

technical field [0001] The invention belongs to the technical field of medicine, relates to a preparation method of medicine, in particular to a preparation method of anesthesia induction agent and intravenous anesthetic propofol. technical background [0002] Propofol (I), commonly known as diisopropylphenol, is chemically called 2,6-diisopropylphenol, and its English name is 2,6-diisopropylphenol. Its chemical structural formula is as follows: [0003] [0004] Propofol was initially used for antioxidation (Chemist, 1981, 52(4):55), and later this compound was widely used for intravenous anesthesia (J.Med.Chem., 1998, 41:1846). Propofol is a new rapid and short-acting intravenous anesthetic commonly used clinically for induction of anesthesia, maintenance of anesthesia, and sedation of critically ill ICU patients. It has the advantages of fast onset of anesthesia induction, rapid recovery and complete functional recovery, and low incidence of postoperative nausea and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C39/06C07C37/045
Inventor 陈艳明倪成良
Owner 云南龙海天然植物药业有限公司
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