Synthesis method for fospropofol disodium

A technique for fospropofol sodium and a synthetic method, which is applied in the field of fospropofol sodium synthesis, can solve the problems of high toxicity of chloromethyl methyl sulfide, inapplicability to production, and expensive reagents, so as to reduce the synthesis cost and benefit The effect of industrial production and short reaction route

Inactive Publication Date: 2012-04-04
SHANGHAI RECORD PHARM CO LTD +1
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  • Claims
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AI Technical Summary

Problems solved by technology

[0006] The route of this method is relatively long, and chloromethyl methyl sulfide has higher toxicity, and reagent is expensive, is not suitable for production

Method used

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Experimental program
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Embodiment Construction

[0019] Below in conjunction with specific embodiment further illustrate how the present invention is realized:

[0020] step one:

[0021] Add 1.2g of solid sodium hydroxide and 9.9g of bromochloromethane (molecular weight 129.38) to a tetrahydrofuran solution of propofol (molecular weight 122.17) under nitrogen protection, heat to 30-40°C for 6 hours, then cool to room temperature and filter , the filtrate was concentrated in vacuo to obtain 3.2 grams of light yellow oil 2-chloromethoxy-1,3-diisopropylbenzene, the yield was 93%, and the equivalent ratio of bromochloromethane and propofol was (5-7) :1, preferably 5:1.

[0022] Step two:

[0023] Dissolve 3.2 g of 2-chloromethoxy-1,3-diisopropylbenzene in 14.0 g of 60% phosphoric acid, add 9.5 g of triethylamine (molecular weight 101.19) and 4.6 g of tetrabutylammonium bromide (molecular weight 322.37), heated to 90-100°C for 1 hour, then concentrated to remove the solvent, added 100 ml of water, adjusted the pH value to...

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Abstract

The invention relates to a synthesis method for fospropofol disodium. The synthesis method for the fospropofol disodium comprises the following steps of: 1, reacting bromochloromethane with propofol under the action of sodium hydroxide at the temperature of between 30 and 40 DEG C to obtain 2-chloromethoxy-1,3-diisopropyl benzene, wherein the equivalent ratio of the bromochloromethane to the propofol is (5-7):1; 2, reacting the 2-chloromethoxy-1,3-diisopropyl benzene with 60 percent phosphoric acid, adding triethylamine and tetrabutyl ammonium bromide, reacting at the temperature of between 90 and 100 DEG C, and performing treatment by using sodium hydroxide to obtain the fospropofol disodium. The synthesis method has the advantages of low cost, short reaction route, environment friendliness, high purity of the obtained product and the like.

Description

technical field [0001] The invention relates to a synthetic method of fospropofol sodium. Background technique [0002] Fospropofol disodium (fospropofol disodium) represented by compound Ⅰ is clinically used as a sedative-hypnotic agent for adult patients in the course of diagnosis or treatment. The drug is an intravenous injection prepared from compound Ⅱ propofol through two steps . [0003] [0004] I II [0005] There is a method that uses propofol to generate methyl sulfide under the action of chloromethyl methyl sulfide, then reacts with diphenyl phosphate to generate fospropofol diphenyl ester, and finally palladium carbon catalyzed deprotection to obtain the target compound I. [0006] The route of this method is relatively long, and chloromethyl methyl sulfide has higher toxicity, and reagent is expensive, is not suitable for production. [0007] Structural formula III, named: 2,6-bis(1-methylethyl)phenoxy]methanol dihydrogen phosphate disodium salt, mole...

Claims

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Application Information

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IPC IPC(8): C07F9/09
Inventor 张芳江沈建兵
Owner SHANGHAI RECORD PHARM CO LTD
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