A new method for the preparation of the intermediate 1-(6-methylpyridin-3-yl)-2-[4-(methylsulfonyl)phenyl]ethanone of etoricoxib

A kind of technology of methylsulfonyl and methylpyridine, applied in the intermediate 1-(6-methylpyridin-3-yl)-2-[4-(methylsulfonyl)phenyl] for preparing etoricoxib A new frontier for ethyl ketones, able to address issues such as yield loss
CN102898357BActive Publication Date: 2016-07-06F I S FAB ILTALIANA SINTETICI SPA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
F I S FAB ILTALIANA SINTETICI SPA
Publication Date
2016-07-06

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Abstract

The present invention refers to a novel process for the preparation of 1-(6-methylpyridin-3-yl)-2-[4-(methylsulfonyl)phenyl]ethanone, an intermediate of the synthesis of Etoricoxib, an active ingredient on which the Arcoxia drug is based.
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Description

technical field

[0001] The object of the present invention is to provide an intermediate for the preparation of 1-(6-methylpyridin-3-yl)-2-[4-(methylsulfonyl)phenyl]ethanone, a kind of etoricoxib (Etoricoxib) synthesis A method for the body of a medicinal anti-inflammatory active ingredient belonging to the class of COX-2 inhibitors. Background technique

[0002] 1-(6-Methylpyridin-3-yl)-2-[4-(methylsulfonyl)phenyl]ethanone of formula (I) having CASRN221615-75-4:

[0003]

[0004] It is an important intermediate for the synthesis of etoricoxib, which is a part of the class of COX-2 inhibitors and has anti-inflammatory active pharmaceutical ingredients, and has been on the market under the trade name Arcoxia since 2002 Suitable pharmaceutical forms are commercially available.

[0005]

[0006] Examples of the use of such compounds for the synthesis of COX-2 inhibitors are shown in WO9955830, WO9915503 and described by Davies, LanW et al. in Journal of Organic Chemistr...

Claims

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