- Synthesis of the bicyclic dienone core of the antitumor agent ottelione B
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The intramolecular Diels-Alder adduct 12 was converted via dimesylate 20 into dienone 7, which represents the unusual, and apparently quite stable, core of the antitumor agent ottelione B (1).
- Clive, Derrick L. J.,Fletcher, Stephen P.
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- Asymmetric Diels-Alder reactions of N-allenoyloxazolidinones catalyzed by Cu(II)-bis(oxazoline) complexes
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Catalytic asymmetric Diels-Alder reactions of N-allenoyloxazolidinones were investigated. Various chiral metal-bis(oxazoline) and metal-pyridinebis(oxazoline) complexes were screened. Cu(SbF6)2(H2O)2(t-BuBox) wa
- Luanphaisarnnont, Torsak
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- Diastereoselective [2,3]-Sigmatropic Rearrangement of N-Allyl Ammonium Ylides
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A rapid and diastereoselective method was developed for the [2,3]-sigmatropic rearrangement of N-Allyl ammonium ylides, affording products in up to 95percent isolated yields and up to 97:3 dr; most of the desired products were formed within 1 minute. For
- Erkman, Kristin,J?rving, Ivar,Kaabel, Sandra,Kanger, T?nis,Murre, Aleksandra
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p. 4183 - 4197
(2019/11/14)
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- Chiral Bronsted acid-catalyzed asymmetric trisubstituted aziridine synthesis using α-diazoacyl oxazolidinones
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Despite the remarkable advances in catalytic asymmetric aziridinations over the past decades, establishing a general procedure for the stereoselective synthesis of trisubstituted aziridines has remained an elusive goal. Chiral N-triflyl phosphoramide-cata
- Hashimoto, Takuya,Nakatsu, Hiroki,Yamamoto, Kumiko,Maruoka, Keiji
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supporting information; experimental part
p. 9730 - 9733
(2011/09/13)
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- Structure-activity relationships in the binding of chemically derivatized CD4 to gp120 from human immunodeficiency virus
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The first step in HIV infection is the binding of the envelope glycoprotein gp120 to the host cell receptor CD4. An interfacial "Phe43 cavity" in gp120, adjacent to residue Phe43 of gp120-bound CD4, has been suggested as a potential target for therapeutic intervention. We designed a CD4 mutant (D1D2F43C) for site-specific coupling of compounds for screening against the cavity. Altogether, 81 cysteine-reactive compounds were designed, synthesized, and tested. Eight derivatives exceeded the affinity of native D1D2 for gp120. Structure-activity relationships (SAR) for derivatized CD4 binding to gp120 revealed significant plasticity of the Phe43 cavity and a narrow entrance. The primary contacts for compound recognition inside the cavity were found to be van der Waals interactions, whereas hydrophilic interactions were detected in the entrance. This first SAR on ligand binding to an interior cavity of gp120 may provide a starting point for structure-based assembly of small molecules targeting gp120-CD4 interaction.
- Xie, Hui,Ng, Danny,Savinov, Sergey N.,Dey, Barna,Kwong, Peter D.,Wyatt, Richard,Smith III, Amos B.,Hendrickson, Wayne A.
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p. 4898 - 4908
(2008/03/11)
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- A short approach to the bicyclo[4.3.0]nonane fragment of stawamycin
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The bicyclo[4.3.0]nonane (C11-C21) fragment of stawamycin has been prepared by a sequence involving 11 steps (10% overall yield) from methyl (R)-(-)-3-hydroxy-2-methylpropionate. Key steps are a Pd-catalysed Stille coupling reaction
- Dias, Luiz C.,Melgar, Gliseida Z.,Jardim, Luciana S. A.
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p. 4427 - 4431
(2007/10/03)
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- Asymmetric Intramolecular Ene Reaction Catalyzed by a Chiral Titanium Reagent and Synthesis of (-)-ε-Cadinene
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A highly diastereo- and enantio-selective intramolecular ene reaction was developed by employing a chiral titanium reagent generated in situ from TiCl2(OPri)2 and a tartrate-derived chiral 1,4-diol.This reaction afforded masked cyclohexanone an
- Narasaka, Koichi,Hayashi, Yujiro,Shimada, Satoru,Yamada, Jun
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p. 261 - 271
(2007/10/02)
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