51394-43-5Relevant articles and documents
Design and characterization of a heterocyclic electrophilic fragment library for the discovery of cysteine-targeted covalent inhibitors
Keeley,ábrányi-Balogh,Keseru
supporting information, p. 263 - 267 (2019/03/05)
A fragment library of electrophilic small heterocycles was characterized through cysteine-reactivity and aqueous stability tests that suggested their potential as covalent warheads. The analysis of theoretical and experimental descriptors revealed correlations between the electronic properties of the heterocyclic cores and their reactivity against GSH that are helpful in identifying suitable fragments for cysteines with specific nucleophilicity. The most important advantage of these fragments is that they show only minimal structural differences from non-electrophilic counterparts. Therefore, they could be used effectively in the design of targeted covalent inhibitors with minimal influence on key non-covalent interactions.
Cobalt-catalyzed addition of styrylboronic acids to 2-vinylpyridine derivatives
Kobayashi, Tsuneyuki,Yorimitsu, Hideki,Oshima, Koichiro
supporting information; experimental part, p. 669 - 673 (2011/10/09)
Treatment of 2-vinyl nitrogen-containing heteroaromatic compounds with styrylboronic acid in the presence of a cobalt catalyst and a base results in an addition reaction to afford the corresponding 4-phenyl-3-butenyl heteroarenes. The adjacent nitrogen atom is essential for the promotion of the reaction because the nitrogen accelerates the addition of the styryl cobalt species, generated by transmetalation, onto the vinyl group. The reaction represents a rare example of cobalt catalysis in the reactions of organoboronic acids. Accelerated addition: Treatment of 2-vinylpyridine derivatives with styrylboronic acids under cobalt catalysis results in addition reactions. This represents a rare example of the cobalt-catalyzed reaction of organoboronic acids. Cobalt shows catalytic activity similar to rhodium, and catalyzes an unprecedented assembly of organoboronic acids and activated alkenes. Copyright
AMINO-HETEROCYCLIC COMPOUNDS
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Page/Page column 34-35, (2010/08/07)
The invention provides PDE9-inhibiting compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, A, and n are as defined herein. Pharmaceutical compositions containing the compounds of Formula I, and uses thereof in treating neurodegenerative and cognitive disorders, such as Alzheimer's disease and schizophrenia, are also provided.
