Novel intermediate for synthesizing topirastat and its preparation method

A technology of topirax and intermediates, applied in the field of drug synthesis, can solve the problems of long time, low total yield, unfavorable industrialized large-scale production, etc., and achieve the effects of increased yield, low cost, and easy control of industrialization
CN105367490BActive Publication Date: 2019-01-04SHANGHAI INST OF PHARMA IND CO LTD +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANGHAI INST OF PHARMA IND CO LTD
Publication Date
2019-01-04

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Abstract

The present invention provides a new topiroxostat synthesis intermediate 4-(2-(imino(pyridine-4-yl)methyl)hydrazinocarbonyl)pyridine N-oxide (compound VI) and a preparation method thereof, wherein isoniazid N-oxide IV and 4-cyanopyridine V are subjected to a reaction in a suitable solvent under an alcohol alkali condition to obtain the product, the alcohol alkali is selected from sodium methoxide, sodium ethoxide, potassium ethoxide or potassium t-butoxide, and the reaction formula is defined in the specification. According to the present invention, through the compound VI, the gout treating drug topiroxostat can be prepared under the mild and easy industrial control reaction conditions.
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Description

technical field

[0001] The invention belongs to the field of drug synthesis, and in particular relates to a new intermediate for synthesizing the drug topirastat for the treatment of gout, 4-(2-(imino(pyridin-4-yl)methyl)hydrazinecarbonyl)pyridine N-oxide , and a preparation method thereof. Background technique

[0002] Topiroxostat (Topiroxostat), the chemical name is 5-(2-cyano-4-pyridyl)-3-(4-pyridyl)-1,2,4-triazole, which is produced by Japan Fuji Pharmaceutical Co., Ltd. A new molecular entity drug developed and launched in Japan for the first time in August 2013. Its trade name is For the treatment of gout, hyperuricemia.

[0003] Chinese patent CN 1561340 discloses a method and route for synthesizing topirastat, see route 1 for details:

[0004]

[0005] This patent route (shown in Route 1) uses isonicotinic acid N-oxide as a raw material, and in the presence of 2-ethoxyl-1-ethoxycarbonyl-1,2-dihydroquinoline (abbreviated as EEDQ) and methanol Esterification t...

Claims

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