4-(1-Pyrrolyl)butanenitrile(4), the key intermediate for the synthesis of 1,2,3,4-tetrahydro-1-indolizinone, was prepared with Clauson-Kass reation. When pyrrole reacted with 4-bromobutanenitrile in PEG-400 dimethyl e...4-(1-Pyrrolyl)butanenitrile(4), the key intermediate for the synthesis of 1,2,3,4-tetrahydro-1-indolizinone, was prepared with Clauson-Kass reation. When pyrrole reacted with 4-bromobutanenitrile in PEG-400 dimethyl ether catalyzed by NaOH, 3-(1-pyrrolyl)butanenitrile was obtained. The nitriles were converted into the corresponding ketones by Hoesch reaction. Some of the ketone derivatives were prepared.展开更多
A simple,highly effective hydrogenation of chiral BINOL to provide H_4-BINOL in multigram scale with good yield（up to 78% yield） was developed.A series of heterogeneous catalysts was tested in the hydrogenation;;the...A simple,highly effective hydrogenation of chiral BINOL to provide H_4-BINOL in multigram scale with good yield（up to 78% yield） was developed.A series of heterogeneous catalysts was tested in the hydrogenation;;the best result was obtained with 5%Pd/ C in EtOH under the H_2 pressure of 50 bar for 2 h.This method is a more useful method for practical synthesis of optically pure H4- BINOL than other available methods.展开更多
文摘4-(1-Pyrrolyl)butanenitrile(4), the key intermediate for the synthesis of 1,2,3,4-tetrahydro-1-indolizinone, was prepared with Clauson-Kass reation. When pyrrole reacted with 4-bromobutanenitrile in PEG-400 dimethyl ether catalyzed by NaOH, 3-(1-pyrrolyl)butanenitrile was obtained. The nitriles were converted into the corresponding ketones by Hoesch reaction. Some of the ketone derivatives were prepared.
基金supported by the Science and Technology Department of Zhejiang Province(no.2008C21041)was partially supported by the NSFC(no.20572101)
文摘A simple,highly effective hydrogenation of chiral BINOL to provide H_4-BINOL in multigram scale with good yield（up to 78% yield） was developed.A series of heterogeneous catalysts was tested in the hydrogenation;;the best result was obtained with 5%Pd/ C in EtOH under the H_2 pressure of 50 bar for 2 h.This method is a more useful method for practical synthesis of optically pure H4- BINOL than other available methods.
