64614-48-8Relevant academic research and scientific papers
Chemo-selective syntheses of: N-t -boc-protected amino ester analogs through Buchwald-Hartwig amination
Karambizi, Victoire G.,O'Brien, Gregory,Rahman, Mahmuda,Scott Goodman, M.,Suwal, Sujit,Wrotny, Matthew
supporting information, p. 2605 - 2608 (2022/02/22)
The synthesis of N-protected amino esters is achieved via a chemo-selective Buchwald Hartwig cross-coupling reaction using PEPPSI-IPr Pd-catalyst. Nearly two dozen functionally and structurally diverse amino ester molecules are created by individually cross-coupling eight aryl halo esters and three different secondary amines. We observed that product formation is more facile in those heterocyclic esters where nitrogen is present ortho to the halo substituent in the heteroaromatic ring. Based on this observation, we propose a possible intermediate step in the cross-coupling cycle, where the nitrogen electron lone pair in the heterocycle may play an important role leading to a higher reaction yield.
Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity
Spanka, Carsten,Glatthar, Ralf,Desrayaud, Sandrine,Fendt, Markus,Orain, David,Troxler, Thomas,Vranesic, Ivo
scheme or table, p. 184 - 188 (2010/04/24)
High throughput screening led to the identification of nicotinamide derivative 2 as a structurally novel mGluR5 antagonist. Optimization of the modular scaffold led to the discovery of 16m, a compound with high affinity for mGluR5 and excellent selectivit
NICOTINIC ACID DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
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Page/Page column 27, (2008/06/13)
The present invention relates to novel nicotinic acid derivatives, of formula (I), wherein the substituents are defined in the specification, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them.
