Preparation method of caspofungin acetate impurity G

Abstract

The invention relates to a preparation method of a caspofungin acetate impurity G. The preparation method comprises the following steps of 1) taking pneumocandin B0 as a raw material, and obtaining a caspofungin acetate impurity G crude product through chemical synthesis; 2) dissolving the caspofungin impurity G crude product with a solvent to prepare a crude product solution, and filtering; 3) separating and purifying the filtered crude product solution through a chromatographic column in a preparation system, and collecting an eluent; and 4) carrying out freeze drying on the qualified eluent to obtain caspofungin acetate impurity G solid powder with the purity of 95% or above. The preparation method comprises the following steps of by taking the intermediate pneumocandin B0 of caspofungin acetate as the raw material, reducing a group at a specific position under the action of a reducing agent to directly obtain the caspofungin acetate impurity G crude product, and then by taking the impurity G crude product as a raw material, obtaining caspofungin acetate impurity G solid powder with the purity of 95% or above through the method for preparing the chromatography, and the requirements of enterprises and markets can be met; and the preparation method is simple in step, stable in condition, high in yield and suitable for large-scale production.

Description

technical field [0001] The invention belongs to the field of chemistry, and in particular relates to a preparation method of caspofungin acetate impurity G. Background technique [0002] Caspofungin acetate is the first echinocandin antifungal drug. It was first approved by the US Food and Drug Administration (FDA) on January 26, 2001. It is mainly used for the treatment of invasive candidiasis and other diseases. Ineffective or intolerable invasive aspergillosis and empirical treatment of neutropenia and suspected fungal infections in patients with fever, as a representative of a new class of echinocandin antibiotics, caspofungin acetate It has the obvious advantages of high selectivity, good antibacterial activity, high safety, and less drug resistance. [0003] Caspofungin acetate is firstly fermented by Glarea Lozoyensis to obtain the fermentation product, and then the fermented product undergoes solid-liquid separation, leaching, adsorption analysis, concentration and ...

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Problems solved by technology

[0008] No other references have specific reports on caspofungin impurity G or caspofungin acetate impurity G at present, and there is no relevant report about preparing high-purity caspofungin acetate impurity G in the prior art, therefore, need to develop A method for preparing high-purity caspofungin acetate impurity G is proposed to meet the needs of the enterprise itself and the market for the reference substance of caspofungin acetate impurity G

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