Synthesis of Conformationally Constrained 5,6,7,8-Tetrahydroimidazo[1,5-a]pyridine Inhibitors of Farnesyltransferase

Autor:	Debra A. McLoughlin, Huff, I.-W. Chen, Kenneth S. Koblan, Baginsky Wf, Christopher J. Dinsmore, Timothy V. Olah, Timothy J. O'Neill, Zartman Cb
Rok vydání:	2000
Předmět:	Models Molecular Pyridines Stereochemistry Farnesyltransferase Molecular Conformation Administration Oral Ring (chemistry) Biochemistry Structure-Activity Relationship chemistry.chemical_compound Dogs In vivo Pyridine Animals Farnesyltranstransferase Enzyme Inhibitors Physical and Theoretical Chemistry Butyraldehyde Alkyl and Aryl Transferases biology Organic Chemistry Farnesyltransferase inhibitor Imidazoles Iminium chemistry biology.protein Indicators and Reagents Amine gas treating
Zdroj:	Organic Letters. 2:3473-3476
ISSN:	1523-7052 1523-7060
Popis:	[reaction: see text] Synthesis of the 8-amino-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine ring system was accomplished by intramolecular cyclization of an iminium ion, derived from condensation of an amine and a substituted gamma-(1-imidazolyl)butyraldehyde. The reaction was used to produce conformationally restricted farnesyltransferase inhibitor analogues which exhibit improved in vivo metabolic stability.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6b4a9be911abd7061880d6f64db23e51 https://doi.org/10.1021/ol0002424 Zobrazit plný text záznamu