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Bortezomib purification method

A technology of bortezomib and purification method, which is applied in the fields of chemical instruments and methods, compounds containing elements of group 3/13 of the periodic table, organic chemistry, etc., can solve the problems of bortezomib with many impurities and reduce production costs, Good dissolution speed, saving manpower and material resources

Inactive Publication Date: 2018-09-25
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] There are many impurities in the finished product of bortezomib obtained by the above synthetic route, and it is necessary to develop a purification method that can reduce impurities in the finished product of bortezomib and improve product quality

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Add a certain amount of crude bortezomib to an appropriate amount of ethyl acetate and heat to 60-65°C to dissolve, and prepare four solutions with concentrations of 300mg / mL, 90mg / mL, 60mg / mL and 30mg / mL respectively, and cool to 25°C Stand still for crystallization for 22 hours, filter to obtain the finished product of bortezomib, take a small amount for liquid phase detection of purity, and weigh the remaining sample after vacuum drying at 30-40°C to calculate the yield.

[0027] serial number

Embodiment 2

[0029] Add a certain amount of crude bortezomib to an appropriate amount of ethyl acetate and heat to 60-65°C to dissolve, and prepare a crystallization solution with a concentration of 60mg / mL, and select 40°C, 30°C, 20°C, 10°C and 0°C respectively Four different crystallization temperatures, static crystallization for 22 hours, filtered to obtain the finished product of bortezomib, a small amount was used for liquid phase detection of purity, and the remaining samples were vacuum-dried at 30-40°C and weighed to calculate the yield.

[0030] serial number

Embodiment 3

[0032] A certain amount of crude bortezomib was added to an appropriate amount of ethyl acetate and heated to 60-65°C to dissolve to prepare a crystallization solution with a concentration of 60mg / mL, and cooled to 20-30°C to stand for crystallization, and to investigate different crystallization times Effect of Team Bortezomib Yield.

[0033] serial number

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Abstract

The invention relates to a bortezomib purification method. The bortezomib is recrystallized in ethyl acetate to prepare bortezomib at a high purity. According to the method, bortezomib production efficiency is improved, production cost is lowered, and the bortezomib purification method is suitable for mass production.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a method for crystallization and purification of bortezomib. Background technique [0002] Bortezomib, whose trade name is Velcade, is a new type of antineoplastic drug developed by Millennium Pharmaceutical Company of the United States. The drug is a 26S proteasome inhibitor, which can lead to tumor cell death by blocking the degradation of various proteins that regulate apoptosis and signal transduction in cells. A large number of studies have found that bortezomib is effective in a variety of tumors, especially multiple myeloma, mantle cell lymphoma and other B cell lymphomas (diffuse large B cell type, follicular cell type, small lymphocyte type, etc.) type / chronic lymphocytic leukemia, marginal zone lymphoma), Hodgkin's lymphoma have strong anti-tumor activity. [0003] CN1960996A discloses N-(2-pyrazine carbonyl)-L-phenylalanine and (1S, 2S, 3R, 5S)-pinanediol 1-ammoniu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F5/02
CPCC07F5/025
Inventor 周明杨文彬葛广存
Owner JIANGSU HANSOH PHARMA CO LTD
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