title: A concise synthesis of silanediol-based transition-state isostere inhibitors of proteases.
abstract: [reaction: see text] An efficient synthesis of silanediol-based transition-state inhibitors of proteases is described. A new convergent synthesis has been optimized by using a two-step sequence of hydrosilylation followed by the addition of a silyllithio species to an imine. The method should be applicable to the synthesis of a wide variety of silanediol isosteres to probe the utility of this unique transition-state isostere.
authors.affiliation: The Department of Chemistry, York University, Toronto, Ontario M3J 1P3, Canada. organ@yorku.ca
authors.forename: Michael G
authors.initials: MG
authors.lastname: Organ
authors.forename: Christophe
authors.initials: C
authors.lastname: Buon
authors.forename: Carl P
authors.initials: CP
authors.lastname: Decicco
authors.forename: Andrew P
authors.initials: AP
authors.lastname: Combs
mesh_terms: D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D012821:Silanes / Q000737:chemistry*
chemical_list: D011480:Protease Inhibitors; D012821:Silanes