19920-85-5Relevant academic research and scientific papers
Generation of bromophenyllithium reagents from dibromobenzenes and addition to carbonyl and nitrile electrophiles
Caron, Stéphane,Do, Nga M.
, p. 1440 - 1442 (2004)
An evaluation of the mono-lithiation of all three regioisomers of dibromobenzene using n-butylithium was performed. The resulting aryllithium reagents were added to electrophiles such as ketones, aldehydes, nitriles and amides to afford the desired benzylic alcohols or ketones.
Halogen-Lithium Exchange of Sensitive (Hetero)aromatic Halides under Barbier Conditions in a Continuous Flow Set-Up
Weidmann, Niels,Nishimura, Rodolfo H. V.,Harenberg, Johannes H.,Knochel, Paul
supporting information, p. 557 - 568 (2020/09/18)
A halogen-lithium exchange reaction of (hetero)aromatic halides performed in the presence of various electrophiles such as aldehydes, ketones, Weinreb amides, and imines using BuLi as exchange reagent and a commercially available flow set-up is reported. The organolithiums generated in situ were instantaneously trapped with various electrophiles (Barbier conditions) resulting in the formation of polyfunctional (hetero)arenes. This method enables the functionalization of (hetero)arenes containing highly sensitive functional groups such as esters, which are not tolerated in batch conditions.
Diethylaminosulfur trifluoride-mediated intramolecular cyclization of 2-hydroxycycloalkylureas to fused bicyclic aminooxazoline compounds and evaluation of their biochemical activity against β-secretase-1 (BACE-1)
Huestis, Malcolm P.,Liu, Wendy,Volgraf, Matthew,Purkey, Hans E.,Yu, Christine,Wang, Weiru,Smith, Darin,Vigers, Guy,Dutcher, Darrin,Hunt, Kevin W.,Siu, Michael
, p. 5802 - 5807 (2013/10/01)
A series of unique bicyclic aminooxazolines were synthesized and found to exhibit micromolar inhibition of β-secretase-1 (BACE-1). The aminooxazolines were procured by an intramolecular diethylaminosulfur trifluoride (DAST)-mediated ring closure of a benz
BACE INHIBITORS
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Page/Page column 12, (2011/02/15)
The present invention provides BACE inhibitors of Formula I: methods for their use, intermediates, and methods for their preparation.
Potent and selective cathepsin K inhibitors
Shinozuka, Tsuyoshi,Shimada, Kousei,Matsui, Satoshi,Yamane, Takahiro,Ama, Mayumi,Fukuda, Takeshi,Taki, Motohiko,Takeda, Yuko,Otsuka, Eri,Yamato, Michiko,Mochizuki, Shin-ichi,Ohhata, Keiko,Naito, Satoru
, p. 6789 - 6806 (2007/10/03)
A novel series of cathepsin K inhibitors derived from Novartis compound I is described. Optimization of the P1, P3, and P1′ units led to the identification of 4-aminophenoxyacetic acid 24b with an IC50 value of 4.8 nM, which possessed an excell
