Synthesis of conformationally constrained 5,6,7, 8-Tetrahydroimidazo[1,5-a]pyridine inhibitors of farnesyltransferase.
作者信息
Dinsmore C J, Zartman C B, Baginsky W F, O'Neill T J, Koblan K S, Chen I W, McLoughlin D A, Olah T V, Huff J R
机构信息
Departments of Medicinal Chemistry, Cancer Research, and Drug Metabolism, Merck Research Laboratories, P.O. Box 4, West Point, Pennsylvania 19486, USA.
出版信息
Org Lett. 2000 Nov 2;2(22):3473-6. doi: 10.1021/ol0002424.
PMID:11082012
Abstract
[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.
摘要
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