CRF Ligands via suzuki and negishi couplings of 3-pyridyl boronic acids or halides with 2-benzyloxy-4-chloro-3-nitropyridine
摘要:
A series of imidazo[4,5-b]pyridines with a 7-(3-pyridyl) substituent is described as high affinity CRF receptor ligands. Individual analogues were synthesized from key intermediates obtained via palladium-catalyzed coupling of 3-pyridyl zinc or boronic acid organometallic intermediates with 2-benzyloxy-4-chloro-3-nitropyridine 12. (C) 2002 Elsevier Science Ltd. All rights reserved.
[EN] SMALL MOLECULE ACTIVATORS OF NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE (NAMPT) AND USES THEREOF [FR] ACTIVATEURS À PETITES MOLÉCULES DE NICOTINAMIDE PHOSPHORIBOSYLTRANSFÉRASE (NAMPT) ET LEURS UTILISATIONS
Ruthenium Catalyzed Direct Asymmetric Reductive Amination of Simple Aliphatic Ketones Using Ammonium Iodide and Hydrogen
作者:Tamal Ghosh、Martin Ernst、A. Stephen K. Hashmi、Thomas Schaub
DOI:10.1002/ejoc.202000750
日期:2020.8.16
On the direct asymmetric reductive amination of aliphatic ketones to primary amines: By using Ru‐Binaphane as catalyst and NH4I as the amine source, it is possible to aminate prochiral aliphatic ketones with moderate ee values up to 74 %.
Imidazo[4,5-b]pyridines as corticotropin releasing factor receptor ligands
作者:Argyrios G. Arvanitis、Joseph T. Rescinito、Charles R. Arnold、Richard G. Wilde、Gary A. Cain、Jung Hui Sun、Jia-Sheng Yan、Christopher A. Teleha、Lawrence W. Fitzgerald、John McElroy、Robert Zaczek、Paul R. Hartig、Scott Grossman、Stephen P. Arneric、Paul J. Gilligan、Richard E. Olson、David W. Robertson
DOI:10.1016/s0960-894x(02)00833-8
日期:2003.1
A series of high affinity CRF receptor ligands with an imidazo[4,5-b]pyridine core is described. Individual analogues were synthesized and tested in a rat CRF receptor binding assay. The best compounds were further tested in the dog N-in-1 pharmaco-kinetic model to assess plasma levels at 1 mg/kg (po) and in the rat situational anxiety model to assess anxiolytic efficacy at 3 mg/kg (po). The structure-activity relationships for good receptor binding affinity are described herein. (C) 2002 Elsevier Science Ltd. All rights reserved.