1578-62-7Relevant articles and documents
Studies of a diastereoselective electrophilic fluorination reaction employing a cryo-flow reactor
Nakayama, Keiji,Browne, Duncan L.,Baxendale, Ian R.,Ley, Steven V.
, p. 1298 - 1302 (2013/07/27)
The application of meso-scale flow chemistry in research laboratories continues to increase. Here, we report on the use of a modular cryo-flow device as applied to a diastereoselective fluorination process. The reactor can be incorporated into existing flow chemistry setups to permit continuous processing at low temperatures without recourse to cryogenic consumables. Georg Thieme Verlag Stuttgart. New York.
AZEPINE DERIVATIVES AS GAMMA-SECRETASE INHIBITORS
-
Page/Page column 14, (2009/04/25)
Compounds of formula (I), pharmaceutical compositions comprising them, and methods for their use are described.
P3 cap modified Phe*-Ala series BACE inhibitors
Chen, Shu-Hui,Lamar, Jason,Guo, Deqi,Kohn, Todd,Yang, Hsiu-Chiung,McGee, James,Timm, David,Erickson, Jon,Yip, Yvonne,May, Patrick,McCarthy, James
, p. 245 - 250 (2007/10/03)
With the aim of reducing molecular weight and adjusting log D value of BACE inhibitors to more favorable range for BBB penetration and better bioavailability, we synthesized and evaluated several series of P3 cap modified BACE inhibitors obtained via replacement of the P3 NHBoc moiety as seen in 3 with other polar functional groups such as amino, hydroxyl and fluorine. Several promising inhibitors emerging from this P3 cap SAR study (e.g., 15 and 19) demonstrated good enzyme inhibitory potencies (BACE-1 IC50 50 ~1 μM).