Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. 1-Methyl-5-(trifluoromethyl)pyrazole underwent deprotonation and subsequent carboxylation mainly or exclusively at either the 4-position of the heterocycle or at the nitrogen-attached methyl group. COA of Formula: C3H3N3O2.
Xu, Pengfei;Shen, Pei;Wang, Hai;Qin, Lian;Ren, Jie;Sun, Qiushuang;Ge, Raoling;Bian, Jinlei;Zhong, Yi;Li, Zhiyu;Wang, JuBo;Qiu, Zhixia research published 《 Discovery of imidazopyrrolopyridines derivatives as novel and selective inhibitors of JAK2》, the research content is summarized as follows. Herein,the design, synthesis, and structure-activity relationships of a series of imidazopyrrolopyridines derivatives I [R1 = H, cyclopropyl, 2-chlorophenyl, etc.; R2 = cyanomethyl, 4,4,4-trifluorobutyl, (3-(cyanomethyl)-1-ethylsulfonyl-azetidin-3-yl), etc.] that selectively inhibit Janus kinase 2 (JAK2) was described . These screening cascades revealed that I [R1 = H; R2 = 3-cyanopropyl] was a preferred compound, with IC50 values of 10 nM for JAK2. Moreover, I [R1 = H; R2 = 3-cyanopropyl] was a selective JAK2 inhibitor with 19-fold, >30-fold and >30-fold selectivity over JAK1, JAK3 and TYK2 resp. In cytokine-stimulated cell-based assays, I [R1 = H; R2 = 3-cyanopropyl] exhibited a higher JAK2 selectivity over JAK1 isoforms. Indeed, at a dose of 20 mg/kg compound I [R1 = H; R2 = 3-cyanopropyl], pSTAT3 and pSTAT5 expression was reduced to levels comparable to those of control animals untreated with GM-CSF. Addnl., I [R1 = H; R2 = 3-cyanopropyl] showed a relatively good bioavailability (F = 38%), a suitable half-life time (T1/2 = 1.9 h), a satisfactory metabolic stability, suggesting that I [R1 = H; R2 = 3-cyanopropyl] might be a promising inhibitor of JAK2 for further development research for the treatment of MPNs.
2075-46-9, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.
4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., COA of Formula: C3H3N3O2
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics