Method for preparing carfilzomib amorphous crystal

A carfilzomib and amorphous technology, applied in the direction of peptides, etc., can solve the problems of affecting the stability of substances, difficult to remove water, etc., and achieve the effect of easy removal, low moisture content, and favorable industrial production
CN104402973AInactive Publication Date: 2015-03-11CHONGQING TAIHAO PHARM CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
CHONGQING TAIHAO PHARM CO LTD
Publication Date
2015-03-11
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides a method for preparing a carfilzomib amorphous crystal. The method comprises the following steps: dissolving carfilzomib in an organic solvent to obtain a carfilzomib solution; concentrating the carfilzomib solution to obtain the carfilzomib amorphous crystal. The method has the advantages that as the solvent is organic, no water is needed, and the organic solvent is easy to remove during concentration, no residual can be generated in the product, the moisture content is extremely low, no crystal water is formed, and the obtained carfilzomib amorphous crystal is relatively high in stability. The carfilzomib amorphous crystal is prepared by dissolving carfilzomib and directly concentrating and drying the carfilzomib solution, that is, the processes of crystal growth and devitrification are not avoided, so that the obtained carfilzomib crystal is amorphous. Therefore, the method is simple, high in operability, and suitable for large-scale industrialized production.
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Description

technical field

[0001] The invention relates to the technical field of medicinal chemistry, in particular to a method for preparing an amorphous carfilzomib crystal. Background technique

[0002] Carfilzomib (Carfilzomib), the chemical name is (2S)-N-((S)-1-((S)-4-methyl-1-((R)-2-methyloxirane- 2-yl)-1-oxopentan-2-ylcarbamoyl)-2-phenethyl)-2–((S)-2-(2-morpholineacetamido)-4-phenyl Butyramide)-4-methylpentanamide, the trade name is Kyprolis, and the molecular formula is C 40 h 57 N 5 o 7 , has the structure shown in formula I:

[0003]

[0004] Carfilzomib was first produced by Onyx Pharmaceuticals as carfilzomib injection freeze-dried powder, which was approved by the U.S. Food and Drug Administration (FD) on July 20, 2012. Multiple myeloma patients treated with 2 drugs, including bortezomib and immunomodulators. The approval of carfilzomib provides a treatment option for patients with multiple myeloma who have relapsed after treatment with current therapies. In t...

Claims

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