- Palladium-Catalyzed α-Arylation of Silylenol Ethers in the Synthesis of Isoquinolines and Phenanthridines
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A diverse array of isoquinolines and phenanthridines have been accessed by developing a two-step, one-pot method constituting regioselective palladium-catalyzed Kuwajima-Urabe α-arylation of silylenol ethers and acid-mediated deprotection, annulation, and aromatization. Structural diversity in the silylenol ethers leads to three different classes of isoquinolines and phenanthridines from which related natural products can be derived. The synthetic utility of this method by the quick assembly of the natural product trispheridine is also demonstrated.
- Saini, Gaurav,Kumar, Pravin,Kumar, Gangam Srikanth,Mangadan, Arun Raj Kizhakkayil,Kapur, Manmohan
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p. 441 - 444
(2018/01/28)
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- Α 7 as intranuclear hydroxynicotinic acetylcholine receptor quinuclidines compd.
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PROBLEM TO BE SOLVED: To provide ligands for the nicotinic α-7 receptor used for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.SOLUTION: The disclosure provides compounds of the specified formula I, including their salts, and compositions and methods using the compounds.
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Paragraph 0715; 0717
(2018/10/03)
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- Synthesis of a unique isoindoline/tetrahydroisoquinoline-based tricyclic sultam library utilizing a Heck-aza-Michael strategy
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The synthesis of a unique isoindoline- and tetrahydroisoquinoline (THIQ)-containing tricyclic sultam library, utilizing a Heck-aza-Michael (HaM) strategy is reported. Both isoindoline and THIQ rings are installed through a Heck reaction on a vinylsulfonamide, followed by one-pot deprotection and intramolecular aza-Michael reaction. Subsequent cyclization with either paraformaldehyde condensation or 1,1′-carbonyldiimidazole coupling generates a variety of tricyclic sultams. Overall, a 160-member library of these sultams, together with their isoindolines/THIQ and secondary sulfonamides precursors, were constructed using this strategy.
- Zang, Qin,Javed, Salim,Porubsky, Patrick,Ullah, Farman,Neuenswander, Benjamin,Lushington, Gerald H.,Basha, Fatima Z.,Organ, Michael G.,Hanson, Paul R.
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body text
p. 211 - 217
(2012/05/19)
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- Intramolecular homolytic substitution of sulfinates and sulfinamides
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A general and efficient method for the synthesis of cyclic sulfi-nates and sulfinamides based on intra-molecular homolytic substitution (SHi) at the sulfur atom by aryl or alkyl radi-cals is described. Both alkyl and benzo-fused compounds can be accessed di-rectly from easily prepared acyclic pre-cursors. Enantiomerically enriched sulfur-based heterocycles were formed through an SHi process with inversion of configuration at the sulfur atom. Cyclization of prochiral radicals proceeded with varying stereochemical outcomes, depending on the size of the incoming radical. 2-Pyridyl and 2-qui-nolyl radicals led to biaryl compounds, which result from attack onto the ortho position of the arylsulfinate rather than a thiophilic substitution.
- Coulomb, Julien,Certal, Victor,Larraufie, Marie-Helene,Ollivier, Cyril,Corbet, Jean-Pierre,Mignani, Gerard,Fensterbank, Louis,Lacote, Emmanuel,Malacria, Max
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supporting information; experimental part
p. 10225 - 10232
(2010/04/05)
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- NOVEL METHODS AND COMPOSITIONS FOR ALLEVIATING PAIN
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The present invention provides a method for the long-term relief of chronic pain in a subject by activating in the subject an analgesic α-adrenergic receptor in the absence of α-2A receptor activation over a period of at least three days, such that relief of chronic pain is maintained in the absence of continued activation of said receptor. The analgesic α-adrenergic receptor can be, for example, the α-2B receptor.
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