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Method for synthesizing mometasone furoate

A technology of mometasone furoate and a compound is applied in the field of drug synthesis and achieves the effects of simple process, low cost and high yield

Active Publication Date: 2016-04-13
山东锐顺药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Aiming at the many problems existing in the existing synthetic method of mometasone furoate, the invention provides a method for synthesizing mometasone furoate

Method used

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  • Method for synthesizing mometasone furoate
  • Method for synthesizing mometasone furoate
  • Method for synthesizing mometasone furoate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] (1) Preparation of compound 1

[0029] Add 50 g of 9β, 11β-epoxy-17α, 21-dihydroxy-16α-methyl-1,4-pregna (steroid)diene-3,2-dione and 300 ml of pyridine into the reaction kettle. When the temperature of the reaction solution is lowered to -5~5°C, add 30g of p-toluenesulfonyl chloride into the reaction kettle, control the temperature at -5~5°C and react for 9h; pour the reaction solution into 3000ml of water, stir to precipitate solid, and discard the water layer , 380ml of dichloromethane was added to the residue, stirred for 10 minutes, separated, and the aqueous layer was extracted twice with 380ml of dichloromethane. The organic phase was adjusted to pH=6~7 with 1N hydrochloric acid, and the liquid was separated, and the organic phase was adjusted to pH=7~8 with saturated sodium bicarbonate solution; the organic phase was washed with 400ml of saturated saline; when the organic phase was concentrated to dryness, 150ml of dichloromethane was added Methane, 250ml of is...

Embodiment 2

[0037] (1) Preparation of compound 1

[0038]Add 50 g of 9β, 11β-epoxy-17α, 21-dihydroxy-16α-methyl-1,4-pregna (steroid)diene-3,2-dione and 300 ml of pyridine into the reaction kettle. When the temperature of the reaction solution is reduced to -5~5°C, add 15g of methanesulfonyl chloride into the reaction kettle, control the temperature at -5~5°C for 9 hours, and TLC detects that the reaction is complete; pour the reaction solution into 3000ml of water, and stir to precipitate a solid; Discard the water layer, add 380ml of dichloromethane to the residue, stir for 10 minutes, separate the layers, extract the water layer twice with 380ml of dichloromethane; Saturated sodium bicarbonate solution to adjust the pH=7~8; the organic phase was washed with 400ml of saturated saline; the organic phase was concentrated to dryness, and 150ml of dichloromethane was added, and 250ml of isopropyl ether was added dropwise at room temperature, and continued to stir for 3h, filtered, and dried ...

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Abstract

The invention belongs to synthetic methods of medicines, and in particular relates to a method for synthesizing mometasone furoate. According to the method, chlorination is carried out to obtain a compound 2 while an esterification reaction is carried out between a compound 1 and furoyl chloride, and ring opening operation is carried out on the compound 2 in the presence of hydrochloric acid to generate mometasone furoate. According to the method, the defects of long process route, complex reaction system, long consumed time and the like of the original process are effectively overcome. The method provided by the invention is simple in process, mild in reaction condition, high in yield, low in cost, high in quality, and low-price and easily-available in raw and auxiliary materials, and is suitable for industrial production.

Description

technical field [0001] The invention belongs to a method for synthesizing medicines, in particular to a method for synthesizing mometasone furoate. Background technique [0002] Mometasone furoate is a commonly synthesized glucocorticoid, which has anti-inflammatory, anti-allergic, vasoconstrictive, decreased vascular permeability, inhibited cell division and antipruritic effects. , and only use it once a day. Mometasone furoate has a good therapeutic effect on skin diseases that are effectively treated by corticosteroids, such as neurodermatitis, eczema, atopic dermatitis, seborrheic dermatitis and psoriasis caused by skin inflammation and pruritus. The current production process of mometasone furoate has the disadvantages of complicated process and long time consumption. Contents of the invention [0003] Aiming at many problems existing in the existing synthetic methods of mometasone furoate, the invention provides a method for synthesizing mometasone furoate. [000...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J17/00
CPCC07J17/00
Inventor 冯永斌于勇马春丽赵宗玉杨萍
Owner 山东锐顺药业有限公司
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