80366-00-3

Upstream product

• 1670-14-0 benzamidine monohydrochloride 
• 62-23-7 4-nitro-benzoic acid 

Downstream Products

• 80366-01-4 1-(4-nitrobenzoyl)-2-phenyl-4-piperidino-4,5-dihydroimidazole 
• 80821-28-9 (4-Nitro-phenyl)-((4S,5S)-2-phenyl-4,5-di-piperidin-1-yl-4,5-dihydro-imidazol-1-yl)-methanone 
• 28825-12-9 3-phenyl-5-(4'-nitrophenyl)-1,2,4-oxadiazole 

Relevant academic research and scientific papers

A metal-free tandem approach to prepare structurally diverse N-heterocycles: Synthesis of 1,2,4-oxadiazoles and pyrimidinones

A metal-free one-pot approach to the diversity oriented synthesis of N-heterocycles, 1,2,4-oxadiazoles and 2,6 disubstituted pyrimidin-4-ones is described via carboxamidation of amidines with aryl carboxylic acids and aryl propargylic acids. The reactions occur at room temperature forming N-acylamidines which undergo tandem nucleophilic addition-deamination- intramolecular cyclisation to give the corresponding heterocyclic compounds in good to excellent yields. This one pot approach has led to the successful synthesis of the drug lead molecule, ataluren, 3-(5-(2-fluorophenyl)-1,2,4- oxadiazol-3-yl) benzoic acid in two steps. the Partner Organisations 2014.