Method for preparing 6-methylnicotinic acid etoricoxib intermediate and ester thereof
A technology for etoricoxib and intermediates, applied in the field of preparation of etoricoxib intermediate 6-methyl nicotinic acid and its esters, can solve the problems of low yield, high temperature and high pressure, long reaction time, etc. The effect of simplicity and mild reaction conditions
Active Publication Date: 2010-08-25
SHANGHAI HISOAR PHARMA TECH & DEV CO LTD +1
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In short, to produce 6-methylnicotinic acid and its esters using the above-mentioned technology of using 2-methyl-6-ethylpyridine as the raw material, the main equipment is mostly made of titanium alloy with excellent anti-corrosion performance and relatively expensive price, and the reaction time Harsh conditions such as long, low yield or high temperature and high pressure are required, and there is a big problem of potential safety hazards, so a new method for preparing 6-methylnicotinic acid and its esters suitable for industrial production is needed in this area
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The invention relates to a method for preparing 6-methylnicotinic acid etoricoxib intermediate and an ester thereof. The preparation method comprises halogenations, hydrolysis reaction and reducing dehalogenation. The method of the invention is simple in production process and mild in reaction conditions and is suitable for commercial production.
Description
A new method for preparing etorocoxib intermediate-6-methylnicotinic acid and its esters Technical field The present invention belongs to the field of intermediate synthesis of etoricoxib, and particularly relates to a preparation method for synthesizing etoricoxib intermediate 6-methylnicotinic acid and its esters. Background technique Etocoxib is a COX-2 inhibitor developed by Merck. It is mainly used for anti-inflammatory and analgesic clinical applications. Patent WO9955830 (Chinese patent ZL99807550.7) discloses a process for synthesizing etorocoxib through methyl 6-methylnicotinate or 6-methylnicotinic acid. The existing method for synthesizing 6-methylnicotinic acid uses 2-methyl-5-ethylpyridine as a raw material and is prepared by oxidation of potassium permanganate, nitric acid, or ozone and oxygen. Using potassium permanganate process [Chinese Journal of Pharmaceutical Industry, 36(5), 266-267; 2005] to prepare 6-methylnicotinic acid, 3.9kg potassium permanganate an...
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IPC IPC(8): C07D213/80C07D213/803
Inventor 唐鹤苑文秋吴波
Owner SHANGHAI HISOAR PHARMA TECH & DEV CO LTD
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