The Expedient Synthesis of 4,2‘-Difluoro-5‘-(7-trifluoromethyl- imidazo[1,2-a]pyrimidin-3-yl)biphenyl-2-carbonitrile, a GABA α2/3 Agonist

Autor:	Yao-Jun Shi, Bruce S. Foster, Ulf-H. Dolling, Mark Cameron, Joseph E. Lynch
Rok vydání:	2006
Předmět:	Agonist Biphenyl Trifluoromethyl Pyrimidine medicine.drug_class Stereochemistry Organic Chemistry Regioselectivity Ligand (biochemistry) Solvent chemistry.chemical_compound chemistry medicine Physical and Theoretical Chemistry
Zdroj:	Organic Process Research & Development. 10:398-402
ISSN:	1520-586X 1083-6160
DOI:	10.1021/op050217j
Popis:	An expedient regioselective synthesis of a GABA α2/3 agonist 1 is described. The key step is an efficient regioselective palladium-catalyzed coupling of 7-trifluoromethylimidazo[1,2-a]pyrimidine (5) to 5‘-chloro-4,2‘-difluorobiphenyl-2-carbonitrile (15). The efficiency of this step was affected by the choice of solvent, ligand, and tetrabutylammonium salt additive.
Databáze:	OpenAIRE
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