A palladium-catalyzed aromatic esterification reaction of aldehydes with arylboronic acids under an air atmosphere was achieved. This reaction tolerates many functional groups and provides aryl benzoate derivatives with yields ranging from moderate to good. Dioxygen takes part in the reaction and is crucial for this transformation.
Smoke inhalation leads to acute lung injury (ALI), a devastating clinical problem associated with high mortality rates. Suppressor of cytokine signaling-1 (SOCS-1) is a negative regulator of proinflammatory cytokine signaling. We have found that adenoviral gene transfer of SOCS-1 ameliorates smoke inhalation-induced lung injury in C57BL/6 mice. We also found that the release of adenosine triphosphate (ATP) was increased post smoke exposure, while oxidized ATP, an inhibitor of purinergic P2X7 receptor, suppressed smoke-induced NALP3 inflammasome assembly, caspase-1 activation, and K efflux. Similar to oxidized ATP, high protein level of SOCS-1 dampened the formation of NALP3 inflammasome and the activation of caspase-1 and IL-1β induced by smoke exposure in mouse alveolar macrophages. In conclusion, SOCS-1 relieves smoke inhalation-induced pulmonary inflammation and injury by inhibiting NALP3 inflammasome formation.
Reaction of aryl- or heteroarylboronic acids with aldehydes, in the presence of PdCl2 and P(1-Nap)3, afforded carbinol derivatives in good to excellent yields. The efficiency of this reaction was demonstrated by the compatibility with nitro, cyano, acetamido, acetoxy, acetyl, carboxyl, trifluoromethyl, fluoro, and chloro groups and the possibility of involving aliphatic aldehyde or hindered substrates. Moreover, the rigorous exclusion of air/moisture is not required in these transformations.
A novel
method to synthesize 4-alkylpyrimidines by the mechanochemical
magnesium-mediated Minisci reaction of pyrimidine derivatives and
alkyl halides has been reported. The reaction process operates with
a broad substrate scope and excellent regioselectivity under mild
conditions with no requirement of transition-metal catalysts, solvents,
and inert gas protection. The practicality of this protocol has been
demonstrated by the up-scale synthesis, mechanochemical product derivatization,
and antimalarial drug pyrimethamine preparation.
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