Microwave-Enhanced Fischer Reaction: An Efficient One-Pot Synthesis of γ-Carbolines
作者:Yongzhou Hu、Jing Chen、Weiliang Chen
DOI:10.1055/s-2007-992411
日期:2008.1
γ-Carbolines were obtained in a simple one-pot Fischer arting from N-acetyl-3-bromo-4-piperidone hydrobro-reaction starting from N-acetyl-3-bromo-4-piperidone hydrobromide and substituted arylhydrazine hydrochlorides in acidic media under microwave irradiation or by a thermal process. The optimization procedures are reported in detail, and the results from micro-wave processes are compared with conventional
Preparation of sodium-hydrogen exchanger type-1 inhibitors
申请人:——
公开号:US20020082274A1
公开(公告)日:2002-06-27
This invention relates to methods of preparing sodium-hydrogen exchanger type 1 (NHE-1) inhibitors of formula I′
1
intermediates of the NHE-1 inhibitors and a new almost colorless form of the NHE-1 inhibitor N-(5-cyclopropyl-1-quinolin-5-yl-1H-pyrazole-4-carbonyl)-guanidine.
METHODS FOR PREPARING SODIUM-HYDROGEN EXCHANGER TYPE-1 INHIBITORS
申请人:Pfizer Inc.
公开号:US20030119873A1
公开(公告)日:2003-06-26
This invention relates to methods of preparing sodium-hydrogen exchanger type 1 (NHE-1) inhibitors of formula I′
1
and methods of preparing pharmaceutical compositions comprising such NHE-1 inhibitors.
Discovery of zoniporide: A potent and selective sodium–hydrogen exchanger type 1 (NHE-1) inhibitor with high aqueous solubility
作者:Angel Guzman-Perez、Ronald T. Wester、Mary C. Allen、Janice A. Brown、Allan R. Buchholz、Ewell R. Cook、Wesley W. Day、Ernest S. Hamanaka、Scott P. Kennedy、Delvin R. Knight、Paul J. Kowalczyk、Ravi B. Marala、Christian J. Mularski、William A. Novomisle、Roger B. Ruggeri、W.Ross Tracey、Roger J. Hill
DOI:10.1016/s0960-894x(01)00059-2
日期:2001.3
Zoniporide (CP-597,396) is a potent and selective inhibitor of NHE-1, which exhibits high aqueous solubility and acceptable pharmacokinetics for intravenous administration. The discovery, synthesis, activities, and rat and dog pharmacokinetics of this compound are presented. The potency and selectivity of zoniporide may be due to the conformation that the molecule adopts due to the presence of a cyclopropyl and a 5-quinolinyl substituent on the central pyrazole ring of the molecule. (C) 2001 Elsevier Science Ltd. All rights reserved.