A novel one-pot protocol for the synthesis of substituted 2-aminooxazoline from isonitriles and 2-aminoethanol was developed and the reactions involved imidoyl diiodide intermediates,which were generated by mixing iso...A novel one-pot protocol for the synthesis of substituted 2-aminooxazoline from isonitriles and 2-aminoethanol was developed and the reactions involved imidoyl diiodide intermediates,which were generated by mixing isonitriles and iodine in CH_2C1_2 at room temperature.展开更多
We report a practical,light-driven nickel-catalyzed hydrocyanation of alkenes using readily available isonitriles as cyanide surrogates.This method proceeds under mild conditions,tolerates a wide range of functional g...We report a practical,light-driven nickel-catalyzed hydrocyanation of alkenes using readily available isonitriles as cyanide surrogates.This method proceeds under mild conditions,tolerates a wide range of functional groups,and delivers linear alkyl nitriles with high efficiency and excellent regioselectivity.The protocol is broadly applicable,including to the late-stage functionalization of complex,bioactive molecules derived from natural products and pharmaceuticals,providing a direct route to valuable nitrile-containing building blocks and facilitating rapid access to drug-like scaffolds.展开更多
In an analytical study of microbial broths,the actinomycete strain Kitasatospora sp.P07101 was found to produce three new congeners,which were designated hazimycins B(1),C(2),and D(3),together with the previously repo...In an analytical study of microbial broths,the actinomycete strain Kitasatospora sp.P07101 was found to produce three new congeners,which were designated hazimycins B(1),C(2),and D(3),together with the previously reported hazimycin(renamed hazimycin A(4)).The structures of these hazimycins were examined using various spectroscopic methods including nuclear magnetic resonance(NMR),and the results revealed that 1–3 were analogues of hazimycin with the replacement of one of the two isonitrile groups in 4 by an NH-formyl group in 1,the two isonitrile groups and an amide group by two NH-formyl groups and a nitrile group in 2,and the two isonitrile groups and two amide groups by two NH-formyl groups and two nitrile groups in 3.Only hazimycin A exhibited moderate antimicrobial activities against Gram-positive bacteria and Candida albicans.These results indicated that the presence of two isonitrile groups in the hazimycin structure is essential for antimicrobial activity.展开更多
文摘A novel one-pot protocol for the synthesis of substituted 2-aminooxazoline from isonitriles and 2-aminoethanol was developed and the reactions involved imidoyl diiodide intermediates,which were generated by mixing isonitriles and iodine in CH_2C1_2 at room temperature.
基金the financial support provided by the National Natural Science Foundation of China(22471035)Fundamental Research Funds for the Central Universities(2232024A-03,2232024Y-01)the Natural Science Foundation of Shanghai(24ZR1403600).
文摘We report a practical,light-driven nickel-catalyzed hydrocyanation of alkenes using readily available isonitriles as cyanide surrogates.This method proceeds under mild conditions,tolerates a wide range of functional groups,and delivers linear alkyl nitriles with high efficiency and excellent regioselectivity.The protocol is broadly applicable,including to the late-stage functionalization of complex,bioactive molecules derived from natural products and pharmaceuticals,providing a direct route to valuable nitrile-containing building blocks and facilitating rapid access to drug-like scaffolds.
基金supported in part by a Kakenhi Grant 23790020(to Nobuhiro Koyama)a Kitasato University Research Grant for Young Researchers(to Nobuhiro Koyama)
文摘In an analytical study of microbial broths,the actinomycete strain Kitasatospora sp.P07101 was found to produce three new congeners,which were designated hazimycins B(1),C(2),and D(3),together with the previously reported hazimycin(renamed hazimycin A(4)).The structures of these hazimycins were examined using various spectroscopic methods including nuclear magnetic resonance(NMR),and the results revealed that 1–3 were analogues of hazimycin with the replacement of one of the two isonitrile groups in 4 by an NH-formyl group in 1,the two isonitrile groups and an amide group by two NH-formyl groups and a nitrile group in 2,and the two isonitrile groups and two amide groups by two NH-formyl groups and two nitrile groups in 3.Only hazimycin A exhibited moderate antimicrobial activities against Gram-positive bacteria and Candida albicans.These results indicated that the presence of two isonitrile groups in the hazimycin structure is essential for antimicrobial activity.
