Synthesis of 2-Substituted Piperazines via Direct α-Lithiation

Autor:	Martin Berkheij, Dennis J. den Boer, Claudia Sewing, Jan H. van Maarseveen, Wouter I. Iwema Bakker, Jan Willem Terpstra, Lisan van der Sluis, Henk Hiemstra, Adri van den Hoogenband
Přispěvatelé:	Synthetic Organic Chemistry (HIMS, FNWI)
Rok vydání:	2005
Předmět:	Transmetalation Piperazine chemistry.chemical_compound Chemistry Organic Chemistry Drug Discovery Electrophile Organic chemistry General Medicine Biochemistry Combinatorial chemistry
Zdroj:	Tetrahedron Letters, 46(14), 2369-2371. Elsevier
ISSN:	1522-2667 0931-7597 0040-4039
DOI:	10.1002/chin.200530146
Popis:	A novel efficient synthetic route towards the pharmaceutically relevant 2-substituted piperazine class is described. The key step involves α-lithiation of N-Boc piperazines, followed by reaction with several electrophiles. To obtain high yields, in some cases transmetallation to copper after the lithiation step is required.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3a8e56d8273e7515b33df40890bb4f13 https://doi.org/10.1002/chin.200530146 Zobrazit plný text záznamu Full Text from ScienceDirect Plný text