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Synthetic method of beclomethasone dipropionate

A technology of dipropionate and beclomethasone, applied in the field of synthesis of beclomethasone dipropionate in aqueous solution of gluconic acid

Active Publication Date: 2015-04-29
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] The reason for not using the simpler method is mainly due to the fact that beclomethasone (CAS: 4419-39-0) has hydroxyl groups at the 11, 17, and 21 positions respectively, and the three hydroxyl groups are simultaneously esterified when the esterification reaction is carried out at the same time , and cannot selectively hydrolyze the 11-position ester group under the condition that the 17 and 21-position ester groups are retained

Method used

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  • Synthetic method of beclomethasone dipropionate
  • Synthetic method of beclomethasone dipropionate
  • Synthetic method of beclomethasone dipropionate

Examples

Experimental program
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Embodiment 1

[0044] Mix 1mmol of beclomethasone 11,17,21-tripropionate in 50ml of organic solvent and 50% aqueous solution of gluconic acid, and react at the specified temperature until the end of the reaction (1 hour interval between beclomethasone 17,21-dipropionic acid The ester content rises and changes less than 1%), concentrate under reduced pressure until there is no organic solvent smell, cool down to 0°C, and dilute in ice water. Filter and dry to obtain beclomethasone 17,21-dipropionate.

[0045]

Embodiment 2

[0047]Mix 1mmol of beclomethasone 11,17,21-tripropionate in 50ml of organic solvent and 50% aqueous solution of gluconic acid, and react at the specified temperature until the end of the reaction (1 hour interval between beclomethasone 17,21-dipropionic acid The ester content rises and changes less than 1%), concentrate under reduced pressure until there is no organic solvent smell, cool down to 0°C, and dilute in ice water. Filter and dry to obtain beclomethasone 17,21-dipropionate.

[0048]

Embodiment 3

[0050] Mix 1mmol of beclomethasone 11,17,21-tripropionate in 50ml of organic solvent and 50% aqueous solution of glucono-δ-lactone, and react at the specified temperature until the end of the reaction (interval of 1 hour for beclomethasone 17, 21-dipropionate content increase and change less than 1%), concentrated under reduced pressure until there is no organic solvent smell, cooled to 0 ℃, diluted in ice water. Filter and dry to obtain beclomethasone 17,21-dipropionate.

[0051]

[0052]

[0053] The average reaction time in embodiment 3 is extended 2 hours compared with embodiment 2.

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Abstract

The invention relates to a synthetic method of beclomethasone dipropionate. According to the method, beclomethasone 11, 17, 21-tripropionate is taken as the raw material and reacts in an organic solvent with a gluconic acid solution or an aqueous solution of ester capable of being converted into gluconic acid in water to prepare beclomethasone dipropionate.

Description

field of invention [0001] The invention relates to a synthetic method for preparing beclomethasone dipropionate by using beclomethasone 11,17,21-tripropionate as raw material through gluconic acid aqueous solution. Background technique [0002] Beclomethasone dipropionate (CAS: 5534-09-8) is a common glucocorticoid drug. The specific structure is as follows. It can be made into ointment, inhalation and other dosage forms to treat skin diseases, asthma, rhinitis etc. [0003] [0004] Beclomethasone dipropionate was first successfully developed by GlaxoSmithKline in the UK. It was approved by the US FDA in June 1980 and was listed in the British Pharmacopoeia, US Pharmacopoeia, European Pharmacopoeia, Japanese Pharmacopoeia and Chinese Pharmacopoeia. . Because beclomethasone dipropionate aerosol preparation is more effective and economical than oral medicine in controlling the symptoms of allergic rhinitis and treating asthma. In 1986, Teijin Corporation of Japan develo...

Claims

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Application Information

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IPC IPC(8): C07J5/00
CPCC07J5/0076
Inventor 韩昆颖孙亮
Owner TIANJIN JINYAO GRP
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