- Regioselectivity in the intramolecular heck reaction of a series of cyclic sulfonamides: An experimental and computational study
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Regioselectivity in the intramolecular Heck reaction of a series of N-sulfonyl-2,5-dihydro-3-substituted pyrroles was studied. These substrates are unbiased in terms of the formed ring size of the new heterocycle. Results indicate that high levels of regi
- Geoghegan, Kimberly,Evans, Paul,Rozas, Isabel,Alkorta, Ibon
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Read Online
- NRF2 REGULATORS
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The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.
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Page/Page column 519
(2015/07/07)
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- Design, synthesis, and X-ray crystallographic analysis of a novel class of Hiv-1 protease inhibitors
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In the present paper, design, synthesis, X-ray crystallographic analysis, and HIV-1 protease inhibitory activities of a novel class of compounds are disclosed. Compounds 28-30, 32, 35, and 40 were synthesized and found to be inhibitors of the HIV-1 protease. The crucial step in their synthesis involved an unusual endo radical cyclization process. Absolute stereochemistry of the three asymmetric centers in the above compounds have been established to be (4S,2′R,3′S) for optimal potency. X-ray crystallographic analysis has been used to determine the binding mode of the inhibitors to the HIV-1 protease.
- Ganguly, Ashit K.,Alluri, Sesha S.,Caroccia, Danielle,Biswas, Dipshikha,Wang, Chih-Hung,Kang, Eunhee,Zhang, Yong,McPhail, Andrew T.,Carroll, Steven S.,Burlein, Christine,Munshi, Vandna,Orth, Peter,Strickland, Corey
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experimental part
p. 7176 - 7183
(2011/12/04)
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- Selective generation of quaternary all-carbon-centres through Heck-cyclisations: Synthesis of mesembrane
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Described is an observation that the intramolecular Heck reaction of a trisubstituted alkene proceeds with high regioselectivity and leads to the preferential formation of a quaternary all-carbon-centre. This observation was subsequently applied in a short synthesis of (±)-mesembrane. The Royal Society of Chemistry 2010.
- Klein, Johannes E. M. N.,Geoghegan, Kimberly,Meral, Nicolas,Evans, Paul
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supporting information; experimental part
p. 937 - 939
(2010/06/12)
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- Synthesis of polycyclic lactams and sultams by a cascade ring-closure metathesis/isomerization and subsequent radical cyclization
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Starting from readily available substrates, a new one-pot procedure has been devised to prepare polycyclic lactams and sultams. 2-Pyrrolines obtained from N,N-bisallylamides by ring-closure metathesis and subsequent isomerization promoted by ruthenium hyd
- Bressy, Cyril,Menant, Christine,Piva, Olivier
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p. 577 - 582
(2007/10/03)
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