ChemInform Abstract: Synthesis of 3-(Hetero)aryl Tetrahydropyrazolo[3,4-c]pyridines by Suzuki-Miyaura Cross-Coupling Methodology

Autor:	Kevin Blades, Paul D. Kemmitt, William McCoull, Stephanie Dickinson, Jason D. Williams, Gillian M. Lamont, Matthew R. Box, Katrina S. Madden
Rok vydání:	2015
Předmět:	chemistry.chemical_compound chemistry XPhos Aryl Pyridine Organic chemistry General Medicine Pyrazole Pivaloyloxymethyl Medicinal chemistry Trifluoromethanesulfonate
Zdroj:	ChemInform. 46
ISSN:	0931-7597
DOI:	10.1002/chin.201508232
Popis:	A new synthetic route to 3-(heteroaryl) tetrahydropyrazolo[3,4-c]pyridines has been developed that uses the Suzuki–Miyaura cross-coupling of a triflate 6 with (hetero)aryl boronic acids or esters. Using Pd(OAc)2 and XPhos or an XPhos precatalyst, a diverse range of substituents at the C3 position of the tetrahydropyrazolo[3,4-c]pyridine skeleton were prepared. The use of pivaloyloxymethyl and benzyl protection also offers the potential to differentially functionalize the pyrazole and tetrahydropyridine nitrogens.
Databáze:	OpenAIRE
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