《Design, synthesis and biological evaluation of novel N-[4-(2-fluorophenoxy)pyridin-2-yl]cyclopropanecarboxamide derivatives as potential c-Met kinase inhibitors》 was written by Liu, Ju; Gong, Yilin; Shi, Jiantao; Hao, Xuechen; Wang, Yang; Zhou, Yunpeng; Hou, Yunlei; Liu, Yajing; Ding, Shi; Chen, Ye. Quality Control of N,N-Dimethylformamide Dimethyl Acetal And the article was included in European Journal of Medicinal Chemistry in 2020. The article conveys some information:
Three series of novel 4-phenoxypyridine derivatives containing 4-methyl-6-oxo-1,6-dihydropyridazine-3-carboxamide, 5-methyl-4-oxo-1,4-dihydropyridazine-3-carboxamide and 4-methyl-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carboxamide moieties, I [R1 = H, 4-F, 4-Cl, 2-F, 2-Cl, 4-MeO], II [R2 = H, 4-CF3, 3,4-(MeO)2, etc.], and III [R3 = H, 2-F, 3-Cl-4-F, etc.], resp., were synthesized and evaluated for their in-vitro inhibitory activities against c-Met kinase and cytotoxic activities against A549, H460, and HT-29 cancer cell lines. The results indicated that most of the compounds showed moderate to good antitumor activities. The most promising compound, III [R3 = H] (IV) (with c-Met IC50value of 0.016μM) showed remarkable cytotoxicity against A549, H460 and HT-29 cell lines with IC50 values of 1.59μM, 0.72μM and 0.56μM, resp. Their preliminary structure-activity relationship (SARs) studies indicate that linker 4-methyl-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carboxamide was preferred, and electron-withdrawing groups on the terminal Ph rings are beneficial for improving the antitumor activities. Furthermore, colony formation, acridine orange/ethidium bromide (AO/EB) staining, apoptosis, and wound-healing assay of compound IV were performed on HT-29 and/or A549 cell lines. The results came from multiple reactions, including the reaction of N,N-Dimethylformamide Dimethyl Acetal(cas: 4637-24-5Quality Control of N,N-Dimethylformamide Dimethyl Acetal)
N,N-Dimethylformamide Dimethyl Acetal(cas: 4637-24-5) belongs to anime. To avoid the problem of multiple alkylation, methods have been devised for “blocking” substitution so that only one alkyl group is introduced. The Gabriel synthesis is one such method; it utilizes phthalimide, C6H4(CO)2NH, whose one acidic hydrogen atom has been removed upon the addition of a base such as KOH to form a salt.Quality Control of N,N-Dimethylformamide Dimethyl Acetal
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem