Heteroaryl ortho-phenoxyethyl amines have been extensively employed in medicinal chemistry as privileged scaffolds for the design of highly potent and selective ligands. Herein we report an efficient, fast and general method for the synthesis of heteroaryl phenoxyethyl amines via Suzuki cross-coupling. This approach offers the opportunity to obtain a large variety of biaryls incorporating five-membered (thiophene, furan, thiazole, pyrazole, imidazole) or six-membered (pyridine, pyrimidine) heteroaromatic rings for appropriate libraries of ligands. All the compounds presented here have never been synthesized before and a full structural characterization is given.

Synthesis of Heteroaryl ortho-Phenoxyethylamines via Suzuki Cross-Coupling: Easy Access to New Potential Scaffolds in Medicinal Chemistry / Manasieva, Leda Ivanova; Battisti, UMBERTO MARIA; Prandi, Adolfo; Brasili, Livio; Franchini, Silvia. - In: SYNTHESIS. - ISSN 0039-7881. - STAMPA. - 47:23(2015), pp. 3767-3775. [10.1055/s-0035-1560456]

Synthesis of Heteroaryl ortho-Phenoxyethylamines via Suzuki Cross-Coupling: Easy Access to New Potential Scaffolds in Medicinal Chemistry

BATTISTI, UMBERTO MARIA;PRANDI, adolfo;BRASILI, Livio;FRANCHINI, Silvia
2015

Abstract

Heteroaryl ortho-phenoxyethyl amines have been extensively employed in medicinal chemistry as privileged scaffolds for the design of highly potent and selective ligands. Herein we report an efficient, fast and general method for the synthesis of heteroaryl phenoxyethyl amines via Suzuki cross-coupling. This approach offers the opportunity to obtain a large variety of biaryls incorporating five-membered (thiophene, furan, thiazole, pyrazole, imidazole) or six-membered (pyridine, pyrimidine) heteroaromatic rings for appropriate libraries of ligands. All the compounds presented here have never been synthesized before and a full structural characterization is given.
2015
47
23
3767
3775
Synthesis of Heteroaryl ortho-Phenoxyethylamines via Suzuki Cross-Coupling: Easy Access to New Potential Scaffolds in Medicinal Chemistry / Manasieva, Leda Ivanova; Battisti, UMBERTO MARIA; Prandi, Adolfo; Brasili, Livio; Franchini, Silvia. - In: SYNTHESIS. - ISSN 0039-7881. - STAMPA. - 47:23(2015), pp. 3767-3775. [10.1055/s-0035-1560456]
Manasieva, Leda Ivanova; Battisti, UMBERTO MARIA; Prandi, Adolfo; Brasili, Livio; Franchini, Silvia
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11380/1073445
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