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Process for preparing high purity low E type Tamoxifen citrate

A technology of tamoxifen and citrate, applied in the field of chemical and pharmaceutical industry, can solve the problems of difficulty in producing high-purity and low-E-type tamoxifen, low high-purity and the like, and achieves low cost, relatively high separation process, high separation short process effect

Inactive Publication Date: 2006-10-04
SHANGHAI NEW HUALIAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Especially according to the separation method provided by the present invention, high-purity low-E tamoxifen or its citrate can be obtained conveniently, especially high-purity low-type tamoxifen whose content of E-isomer is not more than 0.05% can be obtained conveniently. E-type tamoxifen or its citrate solves the difficulty in producing high-purity and low-E-type tamoxifen or its citrate in the pharmaceutical industry

Method used

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  • Process for preparing high purity low E type Tamoxifen citrate
  • Process for preparing high purity low E type Tamoxifen citrate
  • Process for preparing high purity low E type Tamoxifen citrate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] 10 grams of tamoxifen, the content of the E-isomer is 1.8%. Add it into 200 ml of 0.05% sulfuric acid, heat and stir to dissolve; cool to room temperature, and filter to obtain tamoxifen sulfate with increased Z-isomer content.

[0032] Neutralize with alkali to obtain 8 grams of tamoxifen. Tested according to the method specified in the British Pharmacopoeia (98 edition), the content of the E-isomer is 0.02%.

Embodiment 2

[0034] 10 grams of tamoxifen, the content of the E-isomer is 2.1%. Add it into 200 ml of 1% sulfuric acid, heat and stir to dissolve; cool to room temperature, and filter to obtain tamoxifen sulfate with increased Z-isomer content.

[0035] Neutralize with alkali to obtain 6.8 g of tamoxifen. Tested according to the method specified in the British Pharmacopoeia (98 edition), the content of the E-isomer is 0.01%.

Embodiment 3

[0037] 10 grams of tamoxifen, the content of the E-isomer is 1.5%. Add it into 100 ml of 0.5% hydrochloric acid, heat and stir to dissolve; cool to room temperature, and filter to obtain tamoxifen sulfate with increased Z-isomer content.

[0038] Neutralize with alkali to obtain 7.5 g of tamoxifen. Tested according to the method specified in the British Pharmacopoeia (98 edition), the content of the E-isomer is 0.03%.

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Abstract

The preparation process of high purity low type-E content Tamoxifen citrate includes dissolving Tamoxifen in dilute acid solution for refining and forming salt with citric acid; or dissolving Tamoxifen citrate in alcohol for refining, and can obtain Tamoxifen citrate with content of type-E Tamoxifen citrate isomer not higher than 0.05%. The process has the advantages of simple operation, short separation process and low cost.

Description

[0001] This application is a divisional application. The filing date of the original application is December 3, 1999, the application number is 99124208.4, and the title of the invention is "Preparation method of high-purity and low-E tamoxifen or its citrate". Technical field [0002] The present invention relates to a preparation method of tamoxifen or its citrate, more precisely, a preparation method of high-purity low-E tamoxifen or its citrate, belonging to the field of chemical pharmaceutical industry . Background technique [0003] The chemical name of tamoxifen citrate is: (Z)-2-[4-(1,2-diphenyl-1-butenyl)phenoxy]-N,N-dimethylethyl Amine citrate (1:1) can be used clinically as an anti-breast cancer drug. [0004] At present, the method of producing tamoxifen or its citrate at home and abroad is to obtain the dehydrated product through Grignard and dehydration reactions of α-ethyl deoxybenzoin: [0005] [0006] The dehydrate (i.e. tamoxifen) has two isomers of Z...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C217/54C07C213/10
Inventor 吴建越张承华
Owner SHANGHAI NEW HUALIAN PHARMA