Reference of tert-Butyl carbamateIn 2022 ,《Synthesis and biological evaluation of 4-(pyridine-4-oxy)-3-(tetrahydro-2H-pyran-4-yl)-pyrazole derivatives as novel, potent of ALK5 receptor inhibitors》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Wang, Zhenwei; Zhang, Yan; Wang, Hai; Wang, Xiaowei; Yu, Zhuangzhuang; Zhao, Liwen. The article conveys some information:
A novel series of 4-(pyridine-4-oxy)-3-(tetrahydro-2H-pyran-4-yl)-pyrazole derivatives I [R = 4-[4-(2-hydroxyethyl)piperazin-1-yl]-3-(trifluoromethyl)anilino, (2,2-difluoro-1,3-benzodioxol-5-yl)amino, [2-(3-cyanoazetidin-1-yl)-4-pyridyl]amino, etc.] was synthesized and identified as transforming growth factor type β receptor I (TGF-β R1, also known as activin-like kinase 5 or ALK5) inhibitors. Among them, compound I [R = 4-[4-(2-hydroxyethyl)piperazin-1-yl]-3-(trifluoromethyl)anilino] inhibited ALK5 autophosphorylation and NIH3T3 cell activity with IC50 values of 25 nM and 74.6 nM, resp. Compound I [R = 4-[4-(2-hydroxyethyl)piperazin-1-yl]-3-(trifluoromethyl)anilino] also showed favorable pharmacokinetic profile and ameliorated hERG inhibition. More importantly, 30 mg/kg oral administration of compound I [R = 4-[4-(2-hydroxyethyl)piperazin-1-yl]-3-(trifluoromethyl)anilino] could significantly induced tumor growth inhibition in CT26 xenograft model without obvious toxicity. In the experiment, the researchers used many compounds, for example, tert-Butyl carbamate(cas: 4248-19-5Reference of tert-Butyl carbamate)
tert-Butyl carbamate(cas: 4248-19-5) belongs to anime. Acylation is one of the most important reactions of primary and secondary amines; a hydrogen atom is replaced by an acyl group (a group derived from an acid, such as RCOOH or RSO3H, by removal of ―OH, such as RC(=O)―, RS(O)2―, and so on). Reagents may be acid chlorides (RCOC1, RSO2C1), anhydrides ((RCO)2O), or even esters (RCOOR′); the products are amides of the corresponding acids.Reference of tert-Butyl carbamate
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics