75910-81-5Relevant articles and documents
Arylation of diethyl malonate and ethyl cyanoacetate catalyzed by palladium/di-tert-butylneopentylphosphine
Semmes, Jeffrey G.,Bevans, Stephanie L.,Mullins, C. Haddon,Shaughnessy, Kevin H.
supporting information, p. 3447 - 3450 (2015/02/05)
α-Arylated carbonyl derivatives are important structural motifs in many natural products and pharmaceutically active compounds. Although arylation of simple monocarbonyl compounds is a well-established methodology, metal-catalyzed arylation of β-dicarbonyl derivatives is significantly more challenging. The ability of β-dicarbonyl anions to bind to palladium in a κ2-O,O mode, rather than the κ1-C-bound mode required for bond formation, often results in the deactivation of catalyst systems. The C-bound form of the enolate can be favored through the use of sterically demanding ligands. Herein, we report that the sterically demanding di-tert-butylneopentylphosphine (DTBNpP) ligand in combination with Pd(dba)2 provides an effective catalyst for the coupling of aryl bromides and chlorides with diethyl malonate. The Pd/DTBNpP system also catalyzes the coupling of aryl bromides with ethyl cyanoacetate.
PHENALKYLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY
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Page/Page column 147, (2012/03/09)
The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine
Discovery of 1-arylcarbonyl-6,7-dimethoxyisoquinoline derivatives as glutamine fructose-6-phosphate amidotransferase (GFAT) inhibitors
Qian, Yimin,Ahmad, Mushtaq,Chen, Shaoqing,Gillespie, Paul,Le, Nam,Mennona, Frank,Mischke, Steven,So, Sung-Sau,Wang, Hong,Burghardt Charles,Tannu, Shahid,Conde-Knape, Karin,Kochan, Jarema,Bolin, David
scheme or table, p. 6264 - 6269 (2011/11/29)
Through high throughput screening and subsequent hit identification and optimization, we synthesized a series of 1-arylcarbonyl-6,7- dimethoxyisoquinoline derivatives as the first reported potent and reversible GFAT inhibitors. SAR studies of this class o