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New method for preparing Ciclesonide medication for treating asthma disease

A ciclesonide, pharmaceutical-grade technology, applied in the field of preparing ciclesonide, can solve the problems of cumbersome process, high cost of ciclesonide R type, high product price and the like

Inactive Publication Date: 2005-06-15
CHONGQING PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] Summarizing the above two preparation methods, it can be seen that the first method has a complex process, and the obtained ciclesonide R-type has high cost, low yield, expensive product price, and is not suitable for industrialized production.
The ratio (R / S=97.8 / 2.2) of the epimer of the disclosed product of the second method does not meet the standard for medicinal use

Method used

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  • New method for preparing Ciclesonide medication for treating asthma disease
  • New method for preparing Ciclesonide medication for treating asthma disease
  • New method for preparing Ciclesonide medication for treating asthma disease

Examples

Experimental program
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Effect test

Embodiment

[0035] In a 250ml three-necked flask equipped with agitator, put pregnant-1,4-diene-3,20-dione, 16,17-[(ethylmethylene)bis(oxo)]-11-hydroxyl-21 -(2-Methyl-1-carbonylpropoxy)-, [11β, 16α], that is, 10g (0.021mol) of the raw material of formula (II) and 50ml of nitromethane, form a suspension under stirring, and add 70% dropwise 5.3ml (0.0616mol) of perchloric acid, followed by dropwise addition of 15ml (0.126mol) of cyclohexyl formaldehyde, reacted at room temperature for 2-10 hours, dripped 200ml of 5% potassium carbonate aqueous solution, and caused the solution to be neutral, and an oily solid was obtained. The filtrate was poured off, and about 30 ml of ethanol was added to the obtained oily solid to dissolve it, then spun to dryness, and the solid was collected. About 8.8 g of the ciclesonide product (I) was obtained, and its epimer ratio R / S=98.5 / 1.5. The total yield is about 80%.

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Abstract

A process for preparing the medical Huansuonaide features the aldehyde exchange reaction between the compound shown by formula (B) and cyclohexyl formaldehyde to obtain particular epimer, that is Huansuonaide.

Description

technical field [0001] The present invention relates to a process for the preparation of ciclesonide (I). [0002] The structure of ciclesonide shown in formula I: [0003] [0004] Here, the preparation of ciclesonide is obtained by using formula (II) as a starting material to disperse in a solvent, and under the action of a catalyst, undergo aldehyde exchange with cyclohexyl formaldehyde. [0005] The structure of the starting material shown in formula II: [0006] [0007] Among them, R means C 1 -C 12 straight-chain, branched-chain hydrocarbons, or C 3 -C 5 of cycloalkanes. Background technique [0008] Ciclesonide is a new, non-halogenated inhaled glucocorticoid, which has shown better therapeutic effect and lower side effects than existing therapeutic drugs in the treatment of asthma. [0009] In the structure of ciclesonide, C 22 The chiral carbon is R-type, which constitutes the most critical active group for anti-asthma effect. [0010] DE-4129535 dis...

Claims

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Application Information

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IPC IPC(8): A61K31/58A61P11/06C07J71/00
Inventor 彭瑞娟赖开智
Owner CHONGQING PHARMA RES INST
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