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Preparation method of micafungin derivative side chain intermediate

A technology of micafungin and derivatives, applied in the field of medicine and chemical industry, can solve the problems of high difficulty in industrial production and application, complex process, environmental pollution, etc., and achieve the effects of avoiding a large amount of acid and alkali waste water, shortening the process, and high yield

Inactive Publication Date: 2020-01-31
CHONGQING KANGLE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0019] The technical problem to be solved by the present invention lies in a preparation method of the side chain intermediate of micafungin derivatives, which solves defects such as high difficulty in industrial production and application, serious environmental pollution, complex process, and quality problems

Method used

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  • Preparation method of micafungin derivative side chain intermediate
  • Preparation method of micafungin derivative side chain intermediate
  • Preparation method of micafungin derivative side chain intermediate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Add 35.0g of p-hydroxyacetophenone, 46.6g of 1-bromopentane, 71.0g of anhydrous light potassium carbonate, and 175ml of N,N-dimethylformamide into a 500ml reaction flask in sequence, and store at 60°C under nitrogen protection The reaction was stirred at ~80°C for 5 hours. After the reaction was completed, it was quenched with 250ml of purified water, and then extracted three times with 350ml of n-hexane. The organic layers were combined and the organic solvent was removed by rotary evaporation to obtain an oil (Formula 4). Put all the oil, 55.5g of monomethyl terephthalate, 86.5g of potassium tert-butoxide and 350ml of N,N-dimethylformamide into a 1000ml reaction bottle in sequence, and stir at 10℃~30℃ under the protection of nitrogen React for 5 hours, quench the reaction with 1L of methanol, adjust the pH to 4-5 with concentrated hydrochloric acid, vacuum filter to dryness, wash the filter cake with 350ml of methanol and 500ml of purified water, and dry the filter cak...

Embodiment 2

[0044] Add 35.0g of p-hydroxyacetophenone, 54.8g of 1-chloropentane, 42.6g of anhydrous light potassium carbonate, and 175ml of N,N-dimethylformamide into a 500ml reaction bottle in sequence, and keep it under nitrogen protection at 60°C The reaction was stirred at ~80°C for 4 hours, quenched with 250ml of purified water after the reaction was completed, then extracted three times with 350ml of n-hexane, combined the organic layers and rotary evaporated to remove the organic solvent to obtain an oily substance (Formula 4). Put all the oil, 59.8g of monoethyl terephthalate, 74.2g of sodium tert-butoxide and 350ml of N,N-dimethylformamide into a 1000ml reaction bottle in turn, and stir at 10°C to 30°C under nitrogen protection React for 5 hours, quench the reaction with 1L of methanol, adjust the pH to 4-5 with concentrated hydrochloric acid, vacuum filter to dryness, wash the filter cake with 350ml of methanol and 500ml of purified water, and dry the filter cake in vacuum at 60°...

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Abstract

The invention provides a preparation method of a micafungin derivative side chain intermediate. The method is a preparation method of the micafungin derivative side chain intermediate, and the micafungin derivative side chain intermediate is prepared by directly taking monoterephthalate as a raw material. The process route is greatly shortened, toxic and high-pollution noble metal catalysts are prevented from being prepared and used, impurities difficult to remove are prevented from being generated due to excessive reaction, the process is simple, few equipment is occupied, operation is easy and convenient, and the method is suitable for industrial application.

Description

technical field [0001] The invention belongs to the technical field of medicine and chemical industry, and in particular relates to a preparation method of a side chain intermediate of micafungin derivatives. Background technique [0002] Micafungin, English name: Micafungin, also known as FK463, is a new type of echinocandin antifungal drug obtained by chemical synthesis by modifying the natural product of Coleophoma empetri; bacteria, Candida thermos, Candida krusei and Candida parapsilosis have good inhibitory activity against Aspergillus in vitro, but against Cryptococcus neoformans, Fusarium, Zygomycetes and Trichosporum albajiri No inhibitory activity. Micafungin (Micafungin) was developed by Fujisawa Corporation of Japan and was launched in Japan in December 2002 under the name of Fungusrd. It was certified by the U.S. FDA (Food and Drug Administration) in March 2005. In April 2018, CFDA (China Food and Drug Administration) approved Micafungin Sodium for Injection d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D261/08
CPCC07D261/08
Inventor 张文康杨忠鑫廖德洁沈文晖张朝东蔡中文
Owner CHONGQING KANGLE PHARMA
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