Journal ArticleDOI
Allenyl allylic ethers: synthesis and thermal rearrangements
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TLDR
In this article, the authors apply the sequence halogenation/dehydrohalogenization/isomerization to alkenes 1a-g affords allenyl allylic ethers 5a,c,f,g.Abstract:
Application of the sequence halogenation/dehydrohalogenation/isomerization to alkenes 1a-g affords allenyl allylic ethers 5a-g. Thermal isomerizations of 5a,d,e proceed by Claisen rearrangement, while 5b,c,f,g are transformed by alternate modes of [2+2]cycloaddition involving biradical intermediates of type 19 to polycyclic structures; the variations in these thermal isomerizations are mainly a function of ring sizeread more
Citations
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Journal ArticleDOI
Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis.
Arun K. Ghosh,Prasanth R. Nyalapatla,Satish Kovela,Kanury V. S. Rao,Margherita Brindisi,Heather L. Osswald,Masayuki Amano,Masayuki Amano,Manabu Aoki,Manabu Aoki,Manabu Aoki,Johnson Agniswamy,Yuan-Fang Wang,Irene T. Weber,Hiroaki Mitsuya,Hiroaki Mitsuya +15 more
TL;DR: Two high resolution X-ray structures of inhibitor-bound HIV-1 protease revealed extensive interactions with the backbone atoms of HIV- 1 protease and provided molecular insight into the binding properties of these new inhibitors.
Journal ArticleDOI
Reductive free-radical alkylations and cyclisations mediated by 1-alkylcyclohexa-2,5-diene-1-carboxylic acids
Paul A. Baguley,John C. Walton +1 more
TL;DR: In this article, a range of 1-alkylcyclohexa-2,5-diene-1-carboxylic acids were prepared by Birch reduction of benzoic acid and their efficiency as mediators of alkyl radical chain addition and cyclisation was investigated.
Journal ArticleDOI
Formation of radicals by irradiation of alkyl halides in the presence of triethylamine. Application to the synthesis of (±)-bisabolangelone
TL;DR: In this article, the irradiation of unsaturated halides in the presence of triethylamine leads to the formation of corresponding cyclized products, which are used to synthesize the bicyclic core of (±)-bisabolangelone.
Journal ArticleDOI
A formal synthesis of aflatoxin B2 : a Dötz benzannulation approach
Stephen A. Eastham,Steven P. Ingham,Michael R. Hallett,John M. Herbert,Peter Quayle,James Raftery +5 more
TL;DR: A Dotz benzannulation reaction has been used in the synthesis of the furo[2,3-b]furan core of aflatoxin B2 as mentioned in this paper.
Journal ArticleDOI
Synthesis and Antiapoptotic Activity of a Novel Analogue of the Neutral Sphingomyelinase Inhibitor Scyphostatin
Ralf A. Claus,Annette Wüstholz,Stefan Müller,Clemens L. Bockmeyer,Norman H. Riedel,Ralf Kinscherf,Hans-Peter Deigner +6 more
TL;DR: An evaluation of the biological activity of 14 revealed neutral sphingomyelinase inhibition in several in vivo test systems (monocytes, macrophages, hepatocytes) monitoring antiapoptotic effects and the inversion of phorbolester‐induced translocation of green fluorescent protein labelled kinase (protein kinase C‐α).
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