29107-82-2Relevant 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.
Substituted (aryl, heteroaryl, arylmethyl or heteroarylmethyl) hydroxamic acid compounds
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, (2008/06/13)
This invention is directed to compounds of formula I: wherein the variables are as described herein. Compounds within the scope of the present invention possess useful properties, more particularly pharmaceutical properties. They are especially useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. Compounds within the scope of the present invention may also inhibit an MMP, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting MMPs, such disease states involve tissue breakdown and those associated with a physiologically detrimental excess of TNF. The present invention is therefore also directed to the pharmaceutical use of the compounds, pharmaceutical compositions containing the compounds, intermediates leading thereto and methods for the preparation of the compounds and their intermediates.
CONJUGATE ADDITION OF IMIDAZOLINES:A PROTOCOL FOR 1,4-ADDITION TO ENONES AND OTHER ACCEPTORS
Jones, Raymond C. F.,Hirst, Simon C.
, p. 5361 - 5364 (2007/10/02)
The enaminoester 1-benzyl-2-ethoxycarbonylmethyleneimidazolidine reacts with α,β-enones and other Michael acceptors to give 1,4-adducts; removal of the ethoxycarbonyl group completes overall conjugate addition of the imidazoline α-anion (which itself adds 1,2 to enones),and hydrolysis affords carboxylic acids.
