A novel and efficient Ir-catalyzed 1,4-and 1,2-addition of diphenylphosphine oxide to quinolines was developed to obtain various 1,2,3,4-tetrahydroquinoline-2,4-diyl(bisdiphenylphosphine oxide) derivatives. The struct...A novel and efficient Ir-catalyzed 1,4-and 1,2-addition of diphenylphosphine oxide to quinolines was developed to obtain various 1,2,3,4-tetrahydroquinoline-2,4-diyl(bisdiphenylphosphine oxide) derivatives. The structures of these derivatives were characterized by H-RMS and NMR analysis. X-ray crystallography showed that 3 a is in a monoclinic system, space group of P21/c with a = 13.0464(16), b = 12.6244(16), c = 20.210(3)A,β= 105.215(2)o, V =3211.9(7)A^3, Z = 4, F(000)= 1352,μ= 0.42 mm^–1, S = 1.07, the final R = 0.059 and wR = 0.195.The in vitro antitumor activities of target compounds were evaluated by MTT assay against human cancer K562, HL-60, HeLa and BGC-823. The target compounds demonstrated weak or moderate antitumor activity against these cell lines.展开更多
基金Supported by the foundation of the Department of Education of Guangdong Province(2016KTSCX144,2017KZDXM085)Natural Science Foundation of Hunan Province(No.2018JJ3196)the High-level Scientific Research Foundation for the introduction of talent(AL2018008)
文摘A novel and efficient Ir-catalyzed 1,4-and 1,2-addition of diphenylphosphine oxide to quinolines was developed to obtain various 1,2,3,4-tetrahydroquinoline-2,4-diyl(bisdiphenylphosphine oxide) derivatives. The structures of these derivatives were characterized by H-RMS and NMR analysis. X-ray crystallography showed that 3 a is in a monoclinic system, space group of P21/c with a = 13.0464(16), b = 12.6244(16), c = 20.210(3)A,β= 105.215(2)o, V =3211.9(7)A^3, Z = 4, F(000)= 1352,μ= 0.42 mm^–1, S = 1.07, the final R = 0.059 and wR = 0.195.The in vitro antitumor activities of target compounds were evaluated by MTT assay against human cancer K562, HL-60, HeLa and BGC-823. The target compounds demonstrated weak or moderate antitumor activity against these cell lines.
