Zhao, Shizhen; Li, Xinping; Wang, Le; Peng, Wenjing; Ye, Wenling; Li, Weiguo; Wang, Yan-Dong; Chen, Wei-Dong published their research in Bioorganic & Medicinal Chemistry in 2021. The article was titled 《Design, synthesis and evaluation of 1-benzyl-1H-imidazole-5-carboxamide derivatives as potent TGR5 agonists》.Quality Control of Methyl 2-chloro-2-oxoacetate The article contains the following contents:
A series of novel 1-benzyl-1H-imidazole-5-carboxamides I [R1 = 4-methylanilino, 4-fluoro-N-methyl-anilino, 4-phenylpiperazin-1-yl, etc.] and II [R2 = H, 2-Cl, 2,4-di-F, etc.] were designed, synthesized and evaluated in-vitro and in-vivo. The most potent compounds II [R2 = 2,4-di-Cl, 2,5-di-Cl] exhibited excellent agonistic activities against hTGR5, which was superior to those of the reference drugs INT-777 and LCA. In addition, compounds II [R2 = 2,4-di-Cl, 2,5-di-Cl] exhibited good selectivity against FXR and presented significant glucose-lowering effects in-vivo. Compound II [R2 = 2,4-di-Cl] stimulated GLP-1 secretion by activating of TGR5.Methyl 2-chloro-2-oxoacetate(cas: 5781-53-3Quality Control of Methyl 2-chloro-2-oxoacetate) was used in this study.
Methyl 2-chloro-2-oxoacetate(cas: 5781-53-3) belongs to acyl chlorides. In the laboratory, acyl chlorides are generally prepared by treating carboxylic acids with thionyl chloride (SOCl2). The reaction is catalyzed by dimethylformamide and other additives.Quality Control of Methyl 2-chloro-2-oxoacetate
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics