A visible-light-induced decarboxylation coupling/intramolecular cyclization is reported. The one-pot synthesis system provides mild, efficient, and atom economical access to the synthesis of 4-aryl-2-quinolinone derivatives. It is notable that the necessary oxidant in the traditional decarboxylation coupling is replaced by the visible-light irradiation in this paper. In addition, the HBV inhibitor is synthesized by the one-pot synthesis system in an atom economical manner.
The abuse potential of ketamine limits its clinical application, but the precise mechanism remains largely unclear. Here we discovered that ketamine significantly remodels the endocannabinoid-related lipidome and activates 2-arachidonoylglycerol (2-AG) signaling in the dorsal striatum (caudate nucleus and putamen, CPu) of mice. Elevated 2-AG in the CPu is essential for the psychostimulant and reinforcing effects of ketamine, whereas blockade of the cannabinoid CB1 receptor, a predominant 2-AG receptor, attenuates ketamine-induced remodeling of neuronal dendrite structure and neurobehaviors. Ketamine represses the transcription of the monoacylglycerol lipase (MAGL) gene by promoting the expression of PRDM5, a negative transcription factor of the MAGL gene, leading to increased 2-AG production. Genetic overexpression of MAGL or silencing of PRDM5 expression in the CPu robustly reduces 2-AG production and ketamine effects. Collectively, endocannabinoid signaling plays a critical role in mediating the psychostimulant and reinforcing properties of ketamine.
Ap rotocol for the Cu(TFA) 2 -catalyzed( TFA = trifluoroacetic acid) picolinamido-directedC 8 ÀHc yanation of naphthalene derivatives with benzoyl cyanide as the cyano source has been developed. As eries of 8-cyano-1-(picolinamido)naphthalene derivatives were efficiently obtained in moderate to good yields by using this method. We prepared at otal of 22 products, 10 of which have not previously been reported. Benzoyl cyanide was originally employed for the C(sp 2 )ÀHc yanation of arenes. The picolinamide moiety served ac riticalr olea st he directing group in this cyanation reactionofnaphthalenes.
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