38430-03-4Relevant articles and documents
Palladium-catalyzed synthesis of α-iminoamides from imidoyl chlorides and a carbamoylsilane
Cunico, Robert F.,Pandey, Rajesh K.
, p. 5344 - 5346 (2005)
A series of pure imidoyl chlorides were converted into α-iminoamides by treatment with a carbamoylsilane under catalysis by palladium(0) complexes.
Amidinyl Radical Formation through Anodic N?H Bond Cleavage and Its Application in Aromatic C?H Bond Functionalization
Zhao, Huai-Bo,Hou, Zhong-Wei,Liu, Zhan-Jiang,Zhou, Ze-Feng,Song, Jinshuai,Xu, Hai-Chao
supporting information, p. 587 - 590 (2017/01/07)
We report herein an atom-economical and sustainable approach to access amidinyl radical intermediates through the anodic cleavage of N?H bonds. The resulting nitrogen-centered radicals undergo cyclizations with (hetero)arenes, followed by rearomatization,
Discovery of an orally available, brain penetrant BACE1 inhibitor that affords robust CNS Aβ reduction
Stamford, Andrew W.,Scott, Jack D.,Li, Sarah W.,Babu, Suresh,Tadesse, Dawit,Hunter, Rachael,Wu, Yusheng,Misiaszek, Jeffrey,Cumming, Jared N.,Gilbert, Eric J.,Huang, Chunli,McKittrick, Brian A.,Hong, Liwu,Guo, Tao,Zhu, Zhaoning,Strickland, Corey,Orth, Peter,Voigt, Johannes H.,Kennedy, Matthew E.,Chen, Xia,Kuvelkar, Reshma,Hodgson, Robert,Hyde, Lynn A.,Cox, Kathleen,Favreau, Leonard,Parker, Eric M.,Greenlee, William J.
supporting information, p. 897 - 902 (2013/01/15)
Inhibition of BACE1 to prevent brain Aβ peptide formation is a potential disease-modifying approach to the treatment of Alzheimer's disease. Despite over a decade of drug discovery efforts, the identification of brain-penetrant BACE1 inhibitors that substantially lower CNS Aβ levels following systemic administration remains challenging. In this report we describe structure-based optimization of a series of brain-penetrant BACE1 inhibitors derived from an iminopyrimidinone scaffold. Application of structure-based design in tandem with control of physicochemical properties culminated in the discovery of compound 16, which potently reduced cortex and CSF Aβ40 levels when administered orally to rats.
