208124-34-9Relevant articles and documents
Formation of Non-Natural α,α-Disubstituted Amino Esters via Catalytic Michael Addition
Teegardin, Kip A.,Gotcher, Lacey,Weaver, Jimmie D.
supporting information, p. 7239 - 7244 (2018/11/25)
The enolate monoanion of amino esters is explored, and the first catalytic Michael addition of α-amino esters is demonstrated. These studies indicate that the acidity of the αC-H is the primary factor determining reactivity. Thus, polyfluorophenylglycine amino esters yield novel α-amino esters in the presence of a catalytic amount of a guanidine-derived base and Michael acceptors. Reactivity requires an acidic N-H, which is accomplished using common protecting groups such as N-Bz, N-Boc, and N-Cbz. Calculations and labeling experiments provide insight into the governing principles in which a key C-to-N proton transfer occurs, resulting in an expansion of the scope to include a number of natural amino esters. The study culminates with a late-stage functionalization of peptidic γ-secretase inhibitor, DAPT.
Synthesis of a tetrahydroimidazo[2',1':2,3]thiazolo[5,4-c]pyridine derivative with Met inhibitory activity
Amat, Mercedes,Koever, Andrea,Jokic, Danica,Lozano, Oscar,Perez, Maria,Landoni, Nicola,Subrizi, Fabiana,Bautista, Jesus,Bosch, Joan
experimental part, p. 145 - 151 (2010/08/07)
A straightforward synthesis of the Met antagonist JLK1360 involving an alkylationcyclocondensation process using aminothiazole 1 and nitrophenacyl bromide 2, reduction of the nitro group, and coupling of the resulting tetracyclic aniline 5 with an appropr
CHEMICAL COMPOUNDS
-
Page/Page column 55-56, (2008/06/13)
The invention provides a new method for treating disorders associated with activation of the Notch signal transduction pathway comprising administering an effective amount of a compound of Formula (I), in free form or in a pharmaceutically acceptable salt