Synthesis method of micafungin side chain intermediate

A kind of technology of micafungin and synthesis method, which is applied in the field of medicine and achieves the effect of simple steps

Inactive Publication Date: 2020-09-01
大桐制药(中国)有限责任公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patented process allows for efficient production of highly pure miconjugene fungi that can be used as an antifungal agent or drug. By performing these processes multiple stages simultaneously, it becomes possible to create more complex molecules like those found naturally occurring compounds such as nikkomycins (NKs).

Problems solved by technology

This patented describes new types of compounds that can be used effectively treat fungal diseases such as those caused by yeast or other microorganisms like cryptocysts. These drugs are called miccins because they target certain enzyme proteins involved with their growth process. However, these molecules may lack specificity towards different organism groups due to differences between them. Therefore, there has been an issue where this type of substance could potentially harm healthy individuals who use its effects on blood clotting system.

Method used

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  • Synthesis method of micafungin side chain intermediate

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Embodiment Construction

[0022] The following will clearly and completely describe the technical solutions in the embodiments of the present invention with reference to the accompanying drawings in the embodiments of the present invention. Obviously, the described embodiments are only some, not all, embodiments of the present invention. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without creative efforts fall within the protection scope of the present invention.

[0023] see figure 1 Shown, the present invention is a kind of synthetic method of micafungin side chain intermediate, specifically comprises the following steps:

[0024] The first step, weigh 50mmol of 4-pentyloxyacetophenone, 51mmol of methyl p-formylbenzoate, 11g of cesium carbonate and 200ml of 55% ethanol aqueous solution into the reaction flask, and heat up to 50°C while stirring , insulated and stirred for 5h, after the reaction was completed, after naturally

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Abstract

The invention discloses a synthesis method of a micafungin side chain intermediate. An important side chain intermediate for synthesizing micafungin can be obtained through only three steps, and the steps are simple. Firstly, 4-pentoxyl acetophenone and methyl p-formylbenzoate as initial raw materials are subjected to an aldol condensation reaction under the action of an alkali catalyst cesium carbonate to obtain an intermediate M1; then, the intermediate M1 and N-hydroxyl p-toluenesulfonamide are cyclized under the action of the alkali catalyst cesium carbonate to obtain an intermediate M2; and finally, transesterification reaction is carried out on the intermediate M2 and 1-hydroxybenzotriazole to obtain the high-purity micafungin side chain intermediate shown in the formula M (See the specification). A brand-new synthesis route is provided, and a foundation is laid for preparation of a final product micafungin.

Description

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Claims

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Application Information

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Owner 大桐制药(中国)有限责任公司
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