349663-40-7Relevant academic research and scientific papers
Synthesis of Arylethylamines via C(sp3)-C(sp3) Palladium-Catalyzed Cross-Coupling
Lippa, Rhys A.,Battersby, David J.,Murphy, John A.,Barrett, Tim N.
, p. 3583 - 3604 (2021/02/27)
Substituted arylethylamines represent a key structural motif in natural, pharmaceutical, and agrochemical compounds. Access to such scaffolds has been the subject of long-standing synthetic interest. Herein, we report the synthesis of such scaffolds via a palladium-catalyzed C(sp3)-C(sp3) coupling between (chloromethyl)aryls and air-/moisture-stable N,N-dialkylaminomethyltrifluoroborate salts. Rapid hit identification was achieved using microscale high-throughput experimentation and was followed by millimolar-scale reaction parameter optimization. A range of structurally and electronically varied arylethylamine products were obtained in moderate to excellent yields (27-96%, >60 examples). The reaction mechanism is proposed to proceed via formation of a trialkylbenzylammonium species prior to oxidative addition.
SPIROALKENE CARBOXAMIDE DERIVATIVES AND THEIR USE AS CHEMOKINE RECEPTOR MODULATORS
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, (2012/10/18)
The present invention is directed to compounds of Formula (I) below, which are antagonists to the chemoattractant cytokine receptor 2 (CCR2), and/or 5 (CCR5), pharmaceutical compositions, and methods for use thereof.
Spiroalkene carboxamide derivatives and their use as chemokine receptor modulators
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, (2012/10/18)
The present invention is directed to compounds of Formula (I) below, which are antagonists to the chemoattractant cytokine receptor 2 (CCR2), and/or 5 (CCR5), pharmaceutical compositions, and methods for use thereof.
Piperidine and piperazine derivatives which function as 5-ht2a receptor antagonists
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, (2008/06/13)
Compounds of the formula I 1in which R1, R2, X, Y and alk are as defined in claim 1, are potent 5-HT2A antagonists and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory
