400729-18-2Relevant academic research and scientific papers
Base-Mediated Radical Borylation of Alkyl Sulfones
Huang, Mingming,Hu, Jiefeng,Krummenacher, Ivo,Friedrich, Alexandra,Braunschweig, Holger,Westcott, Stephen A.,Radius, Udo,Marder, Todd B.
supporting information, (2021/12/02)
A practical and direct method was developed for the production of versatile alkyl boronate esters via transition metal-free borylation of primary and secondary alkyl sulfones. The key to the success of the strategy is the use of bis(neopentyl glycolato) diboron (B2neop2), with a stoichiometric amount of base as a promoter. The practicality and industrial potential of this protocol are highlighted by its wide functional group tolerance, the late-stage modification of complex compounds, no need for further transesterification, and operational simplicity. Radical clock, radical trap experiments, and EPR studies were conducted which show that the borylation process involves radical intermediates.
4-(Phenylsulfonyl)piperidines: Novel, selective, and bioavailable 5-HT2A receptor antagonists
Fletcher, Stephen R.,Burkamp, Frank,Blurton, Peter,Cheng, Susan K. F.,Clarkson, Robert,O'Connor, Desmond,Spinks, Daniel,Tudge, Matthew,Van Niel, Monique B.,Patel, Smita,Chapman, Kerry,Marwood, Rose,Shepheard, Sara,Bentley, Graham,Cook, Gina P.,Bristow, Linda J.,Castro, Jose L.,Hutson, Peter H.,MacLeod, Angus M.
, p. 492 - 503 (2007/10/03)
On the basis of a spirocyclic ether screening lead, a series of acyclic sulfones have been identifed as high-affinity, selective 5-HT2A receptor antagonists. Bioavailability lacking in the parent, 1-(2-(2,4-difluorophenyl)ethyl)-4-(phenylsulfon
