Hu, Xiaohan; Tang, Sheng; Yang, Feiyi; Zheng, Pengwu; Xu, Shan; Pan, Qingshan; Zhu, Wufu published their research in Molecules in 2021. The article was titled 《Design, synthesis, and antitumor activity of olmutinib derivatives containing acrylamide moiety》.Synthetic Route of C4HCl3N2 The article contains the following contents:
Two series of olmutinib derivatives containing an acrylamide moiety I [R1 = 3-NCC6H4NH, 3-MeOC6H4NH, 4-morpholino; R2 = C(O)CH=CH2, C(O)CH=CHMe, C(O)CH=CMe2, etc.; X = CH, N; R3 = H, CH2NMe2, CH2NEt2] were designed and synthesized and their IC50 values against cancer cell lines (A549, H1975, NCI-H460, LO2, and MCF-7) were evaluated. Most of the compounds I exhibited moderate cytotoxic activity against the five cancer cell lines. The most promising compound, I [R1 = 4-morpholinyl, R2 = C(O)CH=CHMe, X = N; R3 = CH2NMe2 (II)] showed not only excellent activity against EGFR kinase but also pos. biol. activity against PI3K kinase. The structure-activity relationship (SAR) suggested that the introduction of dimethylamine scaffolds with smaller spatial structures was more favorable for antitumor activity. Addnl., the substitution of different acrylamide side chains had different effects on the activity of compounds Generally, compounds I [R1 = 3-MeOC6H4NH, R2 = C(O)CH=CHMe, X = CH, R3 = H] and II were confirmed as promising antitumor agents. The results came from multiple reactions, including the reaction of 2,4,6-Trichloropyrimidine(cas: 3764-01-0Synthetic Route of C4HCl3N2)
2,4,6-Trichloropyrimidine(cas: 3764-01-0) is a member of organic chlorides. Almost all organochlorine compounds are synthesized. It is widely used as intermediates, solvents and pesticides of chemical synthetic products.Synthetic Route of C4HCl3N2
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia