Pyrazoles are synthesized by the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Substituted pyrazoles are prepared by condensation of 1,3-diketones with hydrazine (Knorr-type reactions). For example, acetylacetone and hydrazine gives 3,5-dimethylpyrazole. Quality Control of 761446-44-0.
Klug, Dana M.;Mavrogiannaki, Eftychia M.;Forbes, Katherine C.;Silva, Lisseth;Diaz-Gonzalez, Rosario;Perez-Moreno, Guiomar;Ceballos-Perez, Gloria;Garcia-Hernandez, Raquel;Bosch-Navarrete, Cristina;Cordon-Obras, Carlos;Gomez-Linan, Claudia;Saura, Andreu;Momper, Jeremiah D.;Martinez-Martinez, Maria Santos;Manzano, Pilar;Syed, Ali;El-Sakkary, Nelly;Caffrey, Conor R.;Gamarro, Francisco;Ruiz-Perez, Luis Miguel;Gonzalez Pacanowska, Dolores;Ferrins, Lori;Navarro, Miguel;Pollastri, Michael P. research published 《 Lead Optimization of 3,5-Disubstituted-7-Azaindoles for the Treatment of Human African Trypanosomiasis》, the research content is summarized as follows. Neglected tropical diseases such as human African trypanosomiasis (HAT) are prevalent primarily in tropical climates and among populations living in poverty. Historically, the lack of economic incentive to develop new treatments for these diseases has meant that existing therapeutics have serious shortcomings in terms of safety, efficacy, and administration, and better therapeutics are needed. We now report a series of 3,5-disubstituted-7-azaindoles identified as growth inhibitors of Trypanosoma brucei, the parasite that causes HAT, through a high-throughput screen. We describe the hit-to-lead optimization of this series and the development and preclin. investigation of 29d (I), a potent antitrypanosomal compound with promising pharmacokinetic (PK) parameters. This compound was ultimately not progressed beyond in vivo PK studies due to its inability to penetrate the blood-brain barrier (BBB), critical for stage 2 HAT treatments.
Quality Control of 761446-44-0, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., 761446-44-0.
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics