1206801-33-3Relevant articles and documents
Preparation method of pirfenidone
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, (2020/07/28)
The invention discloses a preparation method of pirfenidone. The method comprises the following steps: carrying out reflux on diethyl malonate (or methyl ester) as an initial raw material and 1, 1, 1,3, 3-tetraethoxy-2-methyl propane in the presence of a catalyst zinc chloride and a solvent acetic anhydride for a reaction to obtain diethyl (or methyl) 2-(3-ethoxy-2-methylallyl)malonate, performing cyclization with aniline to obtain ethyl (or methyl) 5-methyl-2-oxo-1-phenyl-1, 2-dihydropyridin-3-formate, performing alkaline hydrolysis to obtain 5-methyl-2-oxo-1-phenyl-1, 2-dihydropyridine-3-formic acid, and finally performing heating decarboxylation to obtain pirfenidone. Starting materials are cheap and easily available, and the structure is stable, although the synthesis steps comprise four steps, the synthesis process is simple to operate, the reaction process and the final product quality control can be effectively guaranteed, the product yield is high, and the method is suitable for large-scale industrial production requirements of bulk drugs.
