92645-04-0Relevant articles and documents
Stereoselective synthesis of cis-1,3-disubstituted cyclobutyl kinase inhibitors
Helal, Christopher J.,Kang, Zhijun,Lucas, John C.,Bohall, Brooks R.
, p. 1853 - 1856 (2007/10/03)
Matrix presented. Two synthetic routes to a series of structurally novel kinase inhibitors containing a cis-1,3-disubstituted cyclobutane are described. The first route utilized addition of 3-aminocyclobutanol to 1,4-dinitroimidazole 5 as the crucial step in preparing 1, whereas the second route employed a novel 1,4-addition of 4-nitroimidazole 18 to in situ generated cyclobutenone 17 as the key reaction. This allowed for a stereoselective and shorter synthesis that eliminated the use of potentially explosive 1,4-dinitroimidazole 5.