- 3-allylation of tert-butyl 4-oxopiperidine-1-carboxylate
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Reaction of tert-butyl 4-oxopiperidine-1-carboxylate dimethylhydrazone with BuLi in the presence of N,N'-dimethylpropylene urea and subsequently with BrCH2CH=CRR' (R=H, Me, Et; R'=CH2Ar) afforded in 50-80% yields the corresponding te
- Moskalenko,Boev
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- Developing the Saegusa-Ito Cyclisation for the Synthesis of Difluorinated Cyclohexenones
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Palladium(II)-catalysed cycloalkenylation (Saegusa-Ito cyclisation) has been used for the first time to transform difluorinated silylenol ethers to difluorinated cycloalkenones under mild conditions. The silylenol ether precursors were prepared in two high-yielding steps from trifluoroethanol, and cyclised in moderate to good yields. A combination of air and copper(I) chloride in acetonitrile gave the turnover of the initial palladium(II) salt, whereas the provision of an oxygen atmosphere ensured more rapid reaction. Annulations required a minimum level of substitution on the chain, but failed when the alkene was substituted. Annelations allowed a range of n,6-bicyclic systems to be prepared and afforded three products, in which heterocycles were fused to the new cyclohexenone. The least substituted system explored underwent cyclisation followed by terminal oxidation to a cyclic enal, which corresponded to a Wacker product of unusual regiochemistry.
- Percy, Jonathan M.,McCarter, Adam W.,Sewell, Alan L.,Sloan, Nikki,Kennedy, Alan R.,Hirst, David J.
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- Visible-Light-Mediated Generation of Nitrogen-Centered Radicals: Metal-Free Hydroimination and Iminohydroxylation Cyclization Reactions
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The formation and use of iminyl radicals in novel and divergent hydroimination and iminohydroxylation cyclization reactions has been accomplished through the design of a new class of reactive O-aryl oximes. Owing to their low reduction potentials, the inexpensive organic dye eosin Y could be used as the photocatalyst of the organocatalytic hydroimination reaction. Furthermore, reaction conditions for a unique iminohydroxylation were identified; visible-light-mediated electron transfer from novel electron donor-acceptor complexes of the oximes and Et3N was proposed as a key step of this process.
- Davies, Jacob,Booth, Samuel G.,Essafi, Stephanie,Dryfe, Robert A. W.,Leonori, Daniele
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supporting information
p. 14017 - 14021
(2016/01/25)
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- ORALLY ACTIVE RENIN INHIBITORS
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This invention relates to compounds of the formula STR1 wherein Q, Z, D, E, R 3, R 4, R 5 and R 6 are defined as below, and the pharmaceutically acceptable salts thereof are disclosed. The compounds are useful as antihypertensive agents.
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- Orally active renin inhibitors
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This invention relates to compounds of the formula wherein Q, Z, D, E, R3, R?, R? and R? are defined as below, and the pharmaceutically acceptable salts thereof are disclosed. The compounds are useful as antihypertensive agents.
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