- Diastereoselective conjugate addition of organocuprates to chiral racemic olefinic amido esters. Formal total synthesis of paroxetine
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The diastereoselective conjugate addition of an organocopper reagent to a chiral racemic olefinic amido ester has been used as the key step in a formal total synthesis of paroxetine.
- Cossy, Janine,Mirguet, Olivier,Gomez Pardo, Domingo,Desmurs, Jean-Roger
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- A short formal synthesis of paroxetine. Diastereoselective cuprate addition to a chiral racemic olefinic amido ester
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A diastereoselective conjugate addition of an organocopper reagent to a chiral racemic olefinic amido ester has been used as the key step in a formal total synthesis of paroxetine.
- Cossy, Janine,Mirguet, Olivier,Gomez Pardo, Domingo,Desmurs, Jean-Roger
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- A Unified Strategy for the Synthesis of Difluoromethyl- And Vinylfluoride-Containing Scaffolds
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Here, we report a general method for the synthesis of quaternary and tertiary difluoromethylated compounds and their vinylfluoride analogues. The strategy, which relies on a two-step sequence featuring a C-selective electrophilic difluoromethylation and either a palladium-catalyzed decarboxylative protonation or a Krapcho decarboxylation, is practical, scalable, and high yielding. Considering the generality of the method and the attractive properties offered by the difluoromethyl group, this approach provides a valuable tool for late-stage functionalization and drug development.
- Duchemin, Nicolas,Buccafusca, Roberto,Daumas, Marc,Ferey, Vincent,Arseniyadis, Stellios
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p. 8205 - 8210
(2019/10/16)
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- SUBSTITUTED PYRAZOLE COMPOUNDS AS SERINE PROTEASE INHIBITORS
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There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin and/or kallikrein, which compounds include substituted pyrazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which diseases or disorders are amenable to treatment or prevention by the inhibition of thrombin and/or kallikrein.
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Paragraph 0262
(2017/05/27)
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- Model studies on the synthesis of madangamine alkaloids. Assembly of the macrocyclic rings
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Using simplified model derivatives, the assembly of the macrocyclic rings of madangamines, including the 13- and 14-membered D rings of madangamines C-E, the all-cis-triunsaturated 15-membered D ring of madangamine A, and the (Z,Z)-unsaturated 11-membered E ring common to madangamines A-E, has been studied.
- Proto, Stefano,Amat, Mercedes,Pérez, Maria,Ballette, Roberto,Romagnoli, Federica,Mancinelli, Andrea,Bosch, Joan
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p. 3916 - 3919
(2012/09/22)
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- A Diels-Alder Approach to Functionalized cis-Hydroisoquinolines. Attempts to Prepare a Tricyclic Core Unit of Manzamine A
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A dihydropyridinone 8 has been synthesized and shown to undergo efficient Lewis-acid mediated Diels-Alder cycloadditions leading to functionalized cis-hydroisoquinoline products such as 11, 13 and 14.Additional manipulations of both the dienophile 8 and a
- Oliveira Imbroisi, Dennis de,Simpkins, Nigel S.
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p. 1815 - 1823
(2007/10/02)
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- A DIELS-ALDER APPROACH TO FUNCTIONALISED CIS-HYDROISOQUINOLINES
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A new substituted 5,6-dihydro-2(1H)-pyridinone participates in highly efficient Diels-Alder reactions to give functionalised cis-hydroisoquinolines suitable for natural product synthesis.
- Imbroisi, Dennis de Oliveira,Simpkins, Nigel S.
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p. 4309 - 4312
(2007/10/02)
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