In 2016,European Journal of Organic Chemistry included an article by Belaroussi, Rabia; El Hakmaoui, Ahmed; Akssira, Mohamed; Guillaumet, Gerald; Routier, Sylvain. Electric Literature of C9H9N3O2. The article was titled 《Regioselective Synthesis of 2,4-Substituted Pyrido[1′,2′:1,5]pyrazolo[3,4-d]pyrimidines through Sequential Pd-Catalyzed Arylation and SNAr Reactions》. The information in the text is summarized as follows:
The synthesis and regioselective functionalization of rare 2,4-disubstituted-pyrido[1′,2′:1,5]pyrazolo[3,4-d]pyrimidine derivatives is reported. C-4 aminations were performed by chlorine nucleophilic substitution SNAr reactions, and their efficiencies were compared with those for direct one-pot amide C-O activation with bromotripyrrolidinophosphonium hexafluorophosphate (PyBroP) as a reagent. The latter method was used to perform palladium-catalyzed C-4 (het)arylation. Finally, two C-4 amino and aryl derivatives were prepared on a large scale and engaged in desulfurative Liebeskind-Srogl-type reactions under microwave irradiation to afford the envisioned compound library. Each step was optimized, and the results are discussed. In the experiment, the researchers used many compounds, for example, Methyl 2-aminopyrazolo[1,5-a]pyridine-3-carboxylate(cas: 1620075-73-1Electric Literature of C9H9N3O2)
Methyl 2-aminopyrazolo[1,5-a]pyridine-3-carboxylate(cas: 1620075-73-1) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. Electric Literature of C9H9N3O2
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics