Preparation method of citric acid toremifene intermediates

A technology of toremifene citrate and its intermediates, which is applied in the field of medicine and chemical industry, and can solve the problem of inability to prepare toremifene citrate intermediates, non-conservation of valence states, and inability to prepare toremifene citrate Intermediates and other problems, to avoid self-condensation reaction, short reaction time, and cost reduction
CN106966911AActive Publication Date: 2017-07-21NINGBO TEAM PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
NINGBO TEAM PHARMA
Publication Date
2017-07-21

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Abstract

The invention relates to a preparation method of citric acid toremifene intermediates 4-[2-(N,N-dimethylamino)ethyoxyl diphenylketone and 1,2-diphenyl-1-[4[2-[2-N,N- dimethylamino]ethoxyl]-1,4-butanediol. The preparation method of the 4-[2-(N,N-dimethylamino)ethyoxyl diphenylketone comprises the steps that 4-hydroxy diphenyl ketone, inorganic alkali, a first solvent and a second solvent are mixed and are stirred at the temperature of 53-58 DEG C for 0.8-2 hours, then cooling is performed to 40 DEG C or below, N,N-dimethylamino chloroethane hydrochloride is added, heating is performed to reach 80-85 DEG C, and stirring reaction is performed for 2-5 hours; cooling is performed to 40 DEG C or below, drinking water is added, stirring is performed to make the mixture layered, and an upper-layer oil phase is taken; the oil phase is washed with 4% sodium hydroxide solution till it is detected through TLC that the 4-hydroxy diphenyl ketone disappears, then washing is performed with drinking water till pH is 8-9; the obtained product is subjected to decompression at the temperature of 55-60 DEG C to evaporate out the solvent, and the citric acid toremifene intermediates 4-[2-(N,N-dimethylamino)ethyoxyl diphenylketone is obtained after cooling.
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Description

technical field

[0001] The invention relates to the field of medicine and chemical industry, in particular to a toremifene citrate intermediate 4-[2-(N,N-dimethylamino)ethoxy]benzophenone and 1,2-diphenyl - a preparation method of 1-[4-[2-(N,N-dimethylamino)ethoxy]phenyl]-1,4-butanediol. Background technique

[0002] Toremifene (Toremifene) is an estrogen receptor antagonist antineoplastic drug developed by Finnish Famos Company in 1983 for the treatment of postmenopausal women with estrogen receptor positive or unknown metastatic breast cancer. Lion & Company is listed in the European Union under the trade name of Fareston. Toremifene is administered orally in the form of citrate. Toremifene is similar in structure and mechanism of action to tamoxifen, and belongs to triarylbutene anti-estrogen drugs. Studies in recent years have found that toremifene citrate is an effective drug for inhibiting Ebola virus.

[0003] 4-[2-(N,N-Dimethylamino)ethoxy]benzophenone (4-(2-(dim...

Claims

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