221076-43-3

Upstream product

• 5203-15-6 4-(2-methylpropoxy)benzonitrile 
• 62-55-5 thioacetamide 
• 767-00-0 4-cyanophenol 

Downstream Products

• 160844-75-7 2-(3-cyano-4-isobutyloxyphenyl)-4-methylthiazole-5-carboxylic acid ethyl ester 
• 923942-34-1 methyl 2-(3-cyano-4-isobutoxyphenyl)-4-methylthiazole-5-carboxylate 
• 1139901-88-4 tert-butyl 2-(3’-cyano-4’-isobutoxyphenyl)-4-methylthiazole-5-carboxylate 
• 163597-57-7 3-cyanoisobutoxybenzothioamide 
• 144060-53-7 febuxostat 

Relevant academic research and scientific papers

Preparation method of febuxostat intermediate, and application thereof in preparation of febuxostat

The invention provides a preparation method of a compound of structural formula II. The method comprises the following steps: 1) reacting a compound of structural formula VII under the action of an alkylating agent and an alkali to obtain a compound of structural formula VI; 2) reacting the compound of structural formula VI to obtain a compound of structural formula V; 3) reacting the compound ofthe structural formula V with urotropine under an acidic condition in the absence of a solvent to obtain a compound of structural formula IV; 4) reacting the compound of the structural formula IV withhydroxylamine hydrochloride in the presence of an alkali, and dehydrating the obtained reaction product to obtain a compound of structural formula III; and 5) performing a ring closing reaction on the compound of the structural formula III and the compound of the structural formula VIII to obtain the compound of structural formula II. The invention also provides an application of the preparationmethod in the synthesis of febuxostat. The method has the advantages of simplicity in operation, high yield, few side reactions and no highly toxic substances, and is suitable for industrial production as a novel method for preparing the febuxostat intermediate. R in the formulas is a C1-C4 alkyl group.

METHOD FOR PRODUCING 4-SUBSTITUTED BENZOTHIOAMIDE DERIVATIVE

Disclosed is a method appropriate for safely, economically and easily producing at a high yield a 4-substituted benzothioamide derivative which is useful as an intermediate in the production of a 2-(3-cyanophenyl)thiazole derivative useful as a drug for gout. Specifically disclosed is a method for producing a 4-substituted benzothioamide derivative represented by formula (A).