Reference of 866837-96-9, These common heterocyclic compound, 866837-96-9, name is Ethyl 5-amino-1-phenyl-1H-pyrazole-3-carboxylate, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
1 -Phenyl-5-(3-phenyl-ureido)-1 H-pyrazole-3-carboxylic acid 145,3mg (3,63mmol, 1 ,2Eq) of a 60%suspension of NaH in mineral oil aresuspended in 25ml of dioxane, 700mg (3,03 mmol) of ethyl 5-am ino-1 -^-fluorophenyl)-. H-pyrazole-3-carboxylate are added and the resulting mixture is stirred for 10 minutes at RT: Then phenylisocanate (360, 6mg, 3,03mmol, 1 Eq) is added and the resulting mixture is heated to 80C for 5hours. After cooling 7ml of 1 M NaOH are added and the resulting mixture is stirred overnight at RT. The solvent is evaporated in vacuo and the obtained crude product is subjected to HPLCchromatography. 257mg (26%) of the pure product are obtained.
Statistics shows that Ethyl 5-amino-1-phenyl-1H-pyrazole-3-carboxylate is playing an increasingly important role. we look forward to future research findings about 866837-96-9.
Reference:
Patent; SANOFI; RUF, Sven; SADOWSKI, Thorsten; HORSTICK, Georg; SCHREUDER, Herman; BUNING, Christian; OLPP, Thomas; WIRTH, Klaus; WO2012/101199; (2012); A1;,
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