- Diverse ortho-C(sp2)-H functionalization of benzaldehydes using transient directing groups
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Pd-catalyzed C-H functionalizations promoted by transient directing groups remain largely limited to C-H arylation only. Herein, we report a diverse set of ortho-C(sp2)-H functionalizations of benzaldehyde substrates using the transient directing group strategy. Without installing any auxiliary directing group, Pd(II)-catalyzed C-H arylation, chlorination, bromination, and Ir(III)-catalyzed amidation, could be achieved on benzaldehyde substrates. The transient directing groups formed in situ via imine linkage can override other coordinating functional groups capable of directing C-H activation or catalyst poisoning, significantly expanding the scope for metal-catalyzed C-H functionalization of benzaldehydes. The utility of this approach is demonstrated through multiple applications, including late-stage diversification of a drug analogue.
- Liu, Xi-Hai,Park, Hojoon,Hu, Jun-Hao,Hu, Yan,Zhang, Qun-Liang,Wang, Bao-Long,Sun, Bing,Yeung, Kap-Sun,Zhang, Fang-Lin,Yu, Jin-Quan
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supporting information
p. 888 - 896
(2017/05/16)
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- NOVEL COMPOUNDS AS ANTAGONISTS OR INVERSE AGONISTS FOR OPIOID RECEPTORS
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This invention relates to novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy.
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Page/Page column 95
(2010/09/07)
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- PHARMACEUTICAL COMPOSITION CONTAINING OPTICALLY ACTIVE COMPOUND HAVING THROMBOPOIETIN RECEPTOR AGONIST ACTIVITY AND INTERMEDIATE THEREOF
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An optically active 4-phenylthiazole derivative having a thrombopoietin receptor agonist activity and a pharmaceutical composition containing the present compound as an active ingredient are created, and a platelet production regulating agent which can be
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Page/Page column 19-20
(2010/06/11)
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- Kinetic studies on the interactions of manganese-porphyrins with peracetic acid. Part 1. Epoxidation of alkenes and hydroxylation of aromatic rings
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The mechanism of peracetic acid interactions with MnIII complexes of meso-tetra(2,6-dichloro-4-R-phenyl)-porphyrins (RTDCPPMnCl; R = CH3O, H, Br, Cl or NO2) in acetonitrile-acetic acid has been studied. Analysis of the kinetic data revealed that both in cis-stilbene epoxidation and naphthalene hydroxylation the first step of the reaction is the reversible formation of an intermediate adduct 'A' between the catalyst and the oxidant. The subsequent irreversible transformation of 'A' with rate constant k2 leads to the formation of two high-valent oxometallo species, [RTDCPPMnV(O)] and supposedly [RTDCPPMnIV(O)]+. These species are in equilibrium and show distinct oxidation abilities towards the substrates.
- Banfi, Stefano,Cavazzini, Marco,Pozzi, Gianluca,Barkanova, Svetlana V.,Kaliya, Oleg L.
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p. 871 - 877
(2007/10/03)
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