Improved L-thyroxine sodium synthesis method

A technology for sodium thyroxine and thyroxine, which is applied in chemical instruments and methods, preparation of organic compounds, organic chemistry, etc., can solve the problems of low yield of oxidative coupling reaction, affecting product cost, etc., so as to reduce unit production cost, The effect of improving production efficiency and improving catalytic activity
CN102199103AActive Publication Date: 2011-09-28靖江市城中村投资建设有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
靖江市城中村投资建设有限公司
Publication Date
2011-09-28

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Abstract

The invention relates to an improved L-thyroxine sodium synthesis method. The method comprises the following steps of: carrying out iodination reaction, N-acidylation reaction, esterification reaction, oxidative coupling reaction and hydrolysis reaction on L-tyrosine used as a raw material to obtain L-thyroxine, and salifying to obtain L-thyroxine sodium. In the oxidative coupling reaction,N-acetyl-3,5-diiodo-L-tyrosine ethyl ester is used as a starting material, manganese chloride or manganese nitrate is used as a catalyst, boric acid is used as a cocatalyst, ethanol is used as a solvent, the pH value of reaction liquid is 8-9, the reaction temperature is 40-50 DEG C, and oxygen is introduced to carry out oxidative coupling reaction for at least 80 hours at normal pressure to obtain N-acetyl-L-tyrosine ethyl ester; and the catalyst is added twice, the addition amount in the first time is at least 60wt% of the total mass of the catalyst, and the mass ratio of the catalyst to the starting material for the oxidative coupling reaction is 0.008-0.012. The improved synthesis method provided by the invention increases the yield and purity of N-acetyl-L-tyrosine ethyl ester and lowers product cost.
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Description

technical field

[0001] The present invention relates to an improved method for synthesizing L-thyroxine sodium, more specifically, the present invention relates to the improvement of key oxidation coupling reaction in the method for synthesizing L-thyroxine sodium. Background technique

[0002] L-thyroxine is an important hormone used in the treatment of human diseases such as hypothyroidism, cretinism, myxoma, thyroid tumor and obesity. In the early days, L-thyroxine was extracted from animal thyroid glands, but the resulting product had low purity and poor optical purity, and the yield was limited by the source of animal thyroid glands. Now the main method of chemical synthesis is used. At present, most of them use L-tyrosine as a raw material to obtain L-thyroxine through iodization, N-acylation, esterification, oxidative coupling reaction, and hydrolysis reaction, and then form a salt to obtain L-thyroxine sodium sodium. The key that affects the product yield and produ...

Claims

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