31558-41-5Relevant articles and documents
5-HT2A/5-HT2C Receptor Pharmacology and Intrinsic Clearance of N-Benzylphenethylamines Modified at the Primary Site of Metabolism
Leth-Petersen, Sebastian,Petersen, Ida N.,Jensen, Anders A.,Bundgaard, Christoffer,B?k, Mathias,Kehler, Jan,Kristensen, Jesper L.
, p. 1614 - 1619 (2016/11/29)
The toxic hallucinogen 25B-NBOMe is very rapidly degraded by human liver microsomes and has low oral bioavailability. Herein we report on the synthesis, microsomal stability, and 5-HT2A/5-HT2C receptor profile of novel analogues of 25B-NBOMe modified at the primary site of metabolism. Although microsomal stability could be increased while maintaining potent 5-HT2 receptor agonist properties, all analogues had an intrinsic clearance above 1.3 L/kg/h predictive of high first-pass metabolism.
Synthesis of murrayaquinone A and analogues via ring-closing C-H arylation
Bedford, Robin B.,Bowen, John G.,Weeks, Amanda L.
, p. 4389 - 4394 (2013/06/26)
A compact synthesis of Murrayaquinone A is reported, based on sequential Buchwald-Hartwig amination/annulative C-H activation followed by oxidation of the intermediate carbazole. The methodology can be readily extended to other analogues with electron-rich quinone rings.
Storable arylpalladium(II) reagents for alkene labeling in aqueous media
Simmons, Rebecca L.,Yu, Robert T.,Myers, Andrew G.
supporting information; experimental part, p. 15870 - 15873 (2011/11/13)
We show that arylpalladium(II) reagents linked to biotin and indocyanine dye residues can be prepared by decarboxylative palladation of appropriately substituted electron-rich benzoic acid derivatives. When prepared under the conditions described, these organometallic intermediates are tolerant of air and water, can be stored for several months in solution in dimethyl sulfoxide, and permit biotin- and indocyanine dye-labeling of functionally complex olefinic substrates in water by Heck-type coupling reactions.