Application In Synthesis of (R)-2,2′,6,6′-Tetramethoxy-4,4′-bis(diphenylphosphino)-3,3′-bipyridine. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: (R)-2,2′,6,6′-Tetramethoxy-4,4′-bis(diphenylphosphino)-3,3′-bipyridine, is researched, Molecular C38H34N2O4P2, CAS is 221012-82-4, about The preparation of bi-functional organophosphine oxides as potential antitumor agents. Author is Lam, Kim-Hung; Chui, Chung-Hin; Gambari, Roberto; Wong, Raymond Siu-Ming; Cheng, Gregory Yin-Ming; Lau, Fung-Yi; Lai, Paul Bo-San; Tong, See-Wai; Chan, Kit-Wah; Wong, Wai-Yeung; Chan, Albert Sun-Chi; Tang, Johnny Cheuk-On.
Following previously reported pyridinyl phosphine oxides as antitumor agents, the com. available C2-axial chiral organophosphine ligand catalysts, such as 2,2′-bis(diphenylphosphino)-1,1′-binaphthyl (BINAP) 1 and 2,2′,6,6′-tetramethoxy-4,4′-bis(diphenylphosphino)-3,3′-bipyridine (P-Phos) 2 as a convenient source for producing organophosphine oxides were targeted as antitumor leads. Their corresponding chiral and racemic bi-phosphine oxides 3 and 4 can be obtained easily through a simple oxidation step with hydrogen peroxide, and their antitumor activities towards human hepatocellular carcinoma Hep3B cell line were reported. It was found that compound 3 shows stronger antitumor activity than that of 4, where axial chirality cannot improve their activity. Further athymic nude mice Hep3B xenograft model demonstrates the attractive in vivo antitumor potential of 3.
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