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
CN1626546AInactive Publication Date: 2005-06-15CHONGQING PHARMA RES INST
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
CHONGQING PHARMA RES INST
Publication Date
2005-06-15
Estimated Expiration
Not applicable · inactive patent

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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.
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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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