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Synthesis method for ciclesonide

A synthesis method, the technology of cyclohexyl formaldehyde, is applied in the field of ciclesonide synthesis, which can solve the problems of complex post-processing, etc., and achieve the effects of convenient post-processing, less waste, and high efficiency

Inactive Publication Date: 2010-10-13
无棣鑫岳化工集团有限公司
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  • Abstract
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Problems solved by technology

The post-reaction processing is more complex

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  • Synthesis method for ciclesonide
  • Synthesis method for ciclesonide
  • Synthesis method for ciclesonide

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Abstract

The invention discloses a synthesis method for ciclesonide with a structure shown as the formula (III). The synthesis method adopts 16 Alpha-hydroxyprednisolone as material with a structure shown as the formula (I) and acidic ionic liquid as solvent and catalyst with a structure shown as the formula (II), and includes the following specific steps that: the 16Alpha-hydroxyprednisolone, isobutyricanhydride, cyclohexanal and the acidic ionic liquid are added into a reaction container together, and react under the temperature condition of 10 DEG C to 100 DEG C, and after sufficient reaction, the obtained reaction liquid is postprocessed, so that the ciclesonide product is obtained. Since the invention adopts the acidic ionic liquid as solvent and catalyst and a one-pot method for preparation, the technique has the advantages of easy operation, high capacity, high efficiency, less three wastes and convenient postprocessing, the ionic liquid can be reused, and therefore the technique is an economic, practical and environment-friendly technique.

Description

(1) Technical field The invention relates to a synthesis method of ciclesonide. (2) Background technology Ciclesonide, English name: (11β, 16α)-16, 17-[[(R)-Cyclo-hexylmethylene]bis(oxy)]11-hydroxy2-21-(2-methyl-1-oxo -propoxy)pregna-1, 4-diene-3, 20-dione. Chemical formula: C 32 h 44 o 7 , Molecular weight: 540. It is a drug for the treatment of asthma, an inhaled glucocorticoid with a new release and distribution mechanism, which can relieve the inflammation of the lungs and airways of patients. The synthetic routes of ciclesonide reported in the literature mainly contain the following two: Above-mentioned synthetic route is all to be raw material with 16α-hydroxy prednisolone, just process order is different, with perchloric acid as reaction catalyst, reacts with 2,2-dimethoxypropane to generate corresponding acetonylidene product; Then cyclo Hexanaldehyde reaction, and then reacted with isobutyric anhydride under the effect of potassium carbonate to generate th...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J71/00
CPCY02P20/54
Inventor 裴文郑洁孙莉杨培风胡香凝丁茂华
Owner 无棣鑫岳化工集团有限公司
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