Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 °C).Pyrazole used as a ligand to prepare organometallic compounds. COA of Formula: C10H17BN2O2.
Gulati, Anmol;Yeung, Charles S.;Lapointe, Blair;Kattar, Solomon D.;Gunaydin, Hakan;Scott, Jack D.;Childers, Kaleen K.;Methot, Joey L.;Simov, Vladimir;Kurukulasuriya, Ravi;Pio, Barbara;Morriello, Greg J.;Liu, Ping;Tang, Haiqun;Neelamkavil, Santhosh;Wood, Harold B.;Rada, Vanessa L.;Ardolino, Michael J.;Yan, Xin Cindy;Palte, Rachel;Otte, Karin;Faltus, Robert;Woodhouse, Janice;Hegde, Laxminarayan G.;Ciaccio, Paul;Minnihan, Ellen C.;DiMauro, Erin F.;Fell, Matthew J.;Fuller, Peter H.;Ellis, J. Michael research published 《 Optimization of brain-penetrant picolinamide derived leucine-rich repeat kinase 2 (LRRK2) inhibitors》, the research content is summarized as follows. The discovery of potent, kinome selective, brain penetrant LRRK2 inhibitors is the focus of extensive research seeking new, disease-modifying treatments for Parkinson′s disease (PD). Herein, we describe the discovery and evolution of a picolinamide-derived lead series. Our initial optimization efforts aimed at improving the potency and CLK2 off-target selectivity of compound 1 by modifying the heteroaryl C-H hinge and linker regions. This resulted in compound 12 which advanced deep into our research operating plan (ROP) before heteroaryl aniline metabolite 14 was characterized as Ames mutagenic, halting its progression. Strategic modifications to our ROP were made to enable early de-risking of putative aniline metabolites or hydrolysis products for mutagenicity in Ames. This led to the discovery of 3,5-diaminopyridine 15 and 4,6-diaminopyrimidine 16 as low risk for mutagenicity (defined by a 3-strain Ames neg. result). Anal. of key matched mol. pairs 17 and 18 led to the prioritization of the 3,5-diaminopyridine sub-series for further optimization due to enhanced rodent brain penetration. These efforts culminated in the discovery of Et trifluoromethyl pyrazole 23 with excellent LRRK2 potency and expanded selectivity vs. off-target CLK2.
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%., COA of Formula: C10H17BN2O2
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics