- Synthesis of rhazinilam through intramolecular arylcyanation of alkenes catalyzed cooperatively by nickel/aluminum
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Intramolecular arylcyanation across a tri-substituted double bond proceeds to give a primary alkyl cyanide product through functionalization of C-CN and allylic C-H bonds and double C-C bond formation in a 1,3-manner by cooperative nickel/AlMe2
- Yamada, Yuuya,Ebata, Shiro,Hiyama, Tamejiro,Nakao, Yoshiaki
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- Synthesis of isoquinolinone-based tricycles as novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors
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The isoquinolinone-based tricyclic compounds were designed and synthesized. Preliminary biological study of these compounds provided potent compounds 17a, 33b, 33c, 33d, and 33g with low nanomolar IC50s against PARP-1 enzyme.
- Chen, Jianyang,Peng, Haixia,He, Jinxue,Huan, Xiajuan,Miao, Zehong,Yang, Chunhao
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p. 2669 - 2673
(2014/06/09)
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- Dissecting the complex recognition interfaces of potent tetrazole- and pyrrole-based anion binders
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Tetrazoles are potent anion binders. We report here a new family of tetrazole-pyrrole-amide hosts that arise when a tetrazole is incorporated as a new binding element alongside the well-known amidopyrrole anion-binding scaffold. In addition to reporting three new, modular synthetic routes that can be used to access these structures, we also report that the new hosts are highly potent binders of chloride. Along the way, we carried out studies of a pyrrole ester control compound that, surprisingly, bound anions almost as strongly as did the amide analogues. This led us to investigate further the relative importance of the amide NH in halide binding. We report that, despite the regular appearance of this close amide NH - -Cl contact in calculated and experimental X-ray structures, the amide NH in this family of anion hosts does not hydrogen bond strongly to chloride in solution.
- Pinter, Thomas,Simhadri, Chakravarthi,Hof, Fraser
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p. 4642 - 4648
(2013/07/05)
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- Pyrrole chemistry. XXIII. The cyanation of substituted pyrroles with chlorosulfonyl isocyanate (CSI). New syntheses of pyrrole-3-carbonitriles
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Chlorosulfonyl isocyanate (CSI) reacts not only with pyrrole itself but with pyrroles having powerful electron-withdrawing groups in the 2-position.Suitable choice of electron-withdrawing groups allows selective 4-substitution of the pyrrole ring.The N-chlorosulfonyl amides formed are readily converted to the corresponding nitriles.The procedure has been used to provide syntheses of pyrrole-3-carbonitrile and its 1-methyl homologue.
- Loader, Charles E.,Anderson, Hugh J.
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p. 2673 - 2676
(2007/10/02)
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