69472-67-9Relevant academic research and scientific papers
Inexpensive Radical Methylation and Related Alkylations of Heteroarenes
Huang, Qi,Zard, Samir Z.
supporting information, p. 1413 - 1416 (2018/03/09)
A simple method for the introduction of a methyl and higher aliphatic group to various heteroarenes using very inexpensive reagents is described. It is based on the radical addition of a carboxylic xanthate followed by decarboxylation. Depending on the heteroarene structure, the decarboxylation can be spontaneous or induced by heating in N,N-dimethylacetamide or N-methyl pyrrolidone in a microwave oven.
Enantioselective synthesis of polycyclic nitrogen heterocycles by Rh-catalyzed alkene hydroacylation: Constructing six-membered rings in the absence of chelation assistance
Du, Xiang-Wei,Ghosh, Avipsa,Stanley, Levi M.
supporting information, p. 4036 - 4039 (2014/08/18)
Catalytic, enantioselective hydroacylations of N-allylindole-2- carboxaldehydes and N-allylpyrrole-2-carboxaldehydes are reported. In contrast to many alkene hydroacylations that form six-membered rings, these annulative processes occur in the absence of
β-nitroacrylates as useful building blocks for the synthesis of alkyl indole-2-carboxylates
Palmieri, Alessandro,Gabrielli, Serena,Maggi, Raimondo,Ballini, Roberto
, p. 128 - 132 (2014/01/06)
Polyfunctionalized alkyl indole 2-carboxylates can be easily synthesized starting form β-nitroacrylates and o-bromoanilines through an addition-elimination process followed by an intramolecular palladium-catalyzed Heck reaction. Georg Thieme Verlag Stuttg
Indole-2-carboxamides as allosteric modulators of the cannabinoid CB 1 receptor
Piscitelli, Francesco,Ligresti, Alessia,La Regina, Giuseppe,Coluccia, Antonio,Morera, Ludovica,Allarà, Marco,Novellino, Ettore,Di Marzo, Vincenzo,Silvestri, Romano
, p. 5627 - 5631 (2012/08/28)
We synthesized new N-phenylethyl-1H-indole-2-carboxamides as the first SAR study of allosteric modulators of the CB1 receptor. The presence of the carboxamide functionality was required in order to obtain a stimulatory effect. The maximum stimulatory activity on CB1 was exerted by carboxamides 13 (EC50 = 50 nM) and 21 (EC50 = 90 nM) bearing a dimethylamino or piperidinyl group, respectively, at position 4 of the phenethyl moiety and a chlorine atom at position 5 of the indole.
