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. Name: 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole.
Drew, Samuel L.;Thomas-Tran, Rhiannon;Beatty, Joel W.;Fournier, Jeremy;Lawson, Kenneth V.;Miles, Dillon H.;Mata, Guillaume;Sharif, Ehesan U.;Yan, Xuelei;Mailyan, Artur K.;Ginn, Elaine;Chen, Jie;Wong, Kent;Soni, Divyank;Dhanota, Puja;Chen, Pei-Yu;Shaqfeh, Stefan G.;Meleza, Cesar;Pham, Amber T.;Chen, Ada;Zhao, Xiaoning;Banuelos, Jesus;Jin, Lixia;Schindler, Ulrike;Walters, Matthew J.;Young, Stephen W.;Walker, Nigel P.;Leleti, Manmohan Reddy;Powers, Jay P.;Jeffrey, Jenna L. research published 《 Discovery of Potent and Selective PI3Kγ Inhibitors》, the research content is summarized as follows. The selective inhibition of the lipid signaling enzyme PI3Kγ constitutes an opportunity to mediate immunosuppression and inflammation within the tumor microenvironment but is difficult to achieve due to the high sequence homol. across the class I PI3K isoforms. Here, we describe the design of a novel series of potent PI3Kγ inhibitors that attain high isoform selectivity through the divergent projection of substituents into both the “selectivity” and “alkyl-induced” pockets within the ATP (ATP) binding site of PI3Kγ. These efforts have culminated in the discovery of 5-[2-amino-3-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidin-5-yl]-2-[(1S)-1-cyclopropylethyl]-7-(trifluoromethyl)-2,3-dihydro-1H-isoindol-1-one (4(I), IC50 = 0.064 μM, THP-1 cells), which displays >600-fold selectivity for PI3Kγ over the other class I isoforms and is a promising step toward the identification of a clin. development candidate. The structure-activity relationships identified throughout this campaign demonstrate that greater γ-selectivity can be achieved by inhibitors that occupy an “alkyl-induced” pocket and possess bicyclic hinge-binding motifs capable of forming more than one hydrogen bond to the hinge region of PI3Kγ.
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%., Name: 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics