Searching for cyclin-dependent kinase inhibitors using a new variant of the cope elimination

…, A Echalier, JA Endicott, IR Hardcastle…

Index: Griffin, Roger J.; Henderson, Andrew; Curtin, Nicola J.; Echalier, Aude; Endicott, Jane A.; Hardcastle, Ian R.; Newell, David R.; Noble, Martin E. M.; Wang, Lan-Zhen; Golding, Bernard T. Journal of the American Chemical Society, 2006 , vol. 128, # 18 p. 6012 - 6013

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Citation Number: 30

Abstract

β-Piperidinoethylsulfides are oxidized by m-chloroperbenzoic acid to intermediates containing both N-oxide and sulfone functions. These undergo a Cope-type elimination to a vinylsulfone that can be captured by amines to afford β-aminoethylsulfones. When a β- aminoethylsulfone group is linked to the 4-position of a phenyl group attached at N-2 of O 6- cyclohexylmethylguanine, the resulting derivatives are inhibitors of the cyclin-dependent ...