反応 #440628

ord-8f779cba557448a3b6eb3b3134ca7157

溶媒

反応条件

詳細条件
See reaction.notes.procedure_details.

実験手順

5-Cyclopropyl-1-(2-chloro-4-methanesulfonylphenyl)-1H-pyrazole-4-carboxylic acid methyl ester is hydrolyzed with a base such as sodium hydroxide in water to form 5-cyclopropyl-1-(2-chloro-4-methanesulfonylphenyl)-1H-pyrazole-4-carboxylic acid, analogous to the formula IX′ acid. The carboxylic acid pyrazole is then activated with coupling agent such as thionyl chloride to form the activated compound, analogous to the formula X′ compound. The activated compound is then coupled with guanidine to form the NHE-1 inhibitor, N-{5-cyclopropyl-1-(2-chloro-4-methanesulfonylphenyl)-1H-pyrazole-4-carbonyl}-guanidine.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US06753334B2uspto-grants-2004_06