- Direct access to 3-aminoindazoles by Buchwald-Hartwig C-N coupling reaction
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An efficient synthesis of various N-substituted 3-aminoindazoles using Buchwald-Hartwig C-N coupling reaction is described. Several parameters were varied, including the nature of the halogen atom and the protecting group of the starting materials, as well as the effects of the catalyst system, base, solvent, and reaction time. The efficiency of microwave versus conventional heating was also compared to test the outcome of the reaction. Thus, by applying this recent knowledge about metal-catalyzed aminations, an alternative for the direct synthesis of primary 3-aminoindazoles has been provided. Georg Thieme Verlag Stuttgart. New York.
- Lohou, Elodie,Collot, Valeri,Stiebing, Silvia,Rault, Sylvain
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experimental part
p. 2651 - 2663
(2011/10/04)
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- Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists
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The synthesis and biological evaluation of novel 3-amino indazole melanin concentrating hormone receptor-1 antagonists are reported, several of which demonstrated functional activity of less than 100 nM. Compounds 19 and 28, two of the more potent compounds identified in this study, were characterized by high exposure in the brain and demonstrated robust efficacy when dosed in diet-induced obese mice.
- Vasudevan, Anil,Souers, Andrew J.,Freeman, Jennifer C.,Verzal, Mary K.,Gao, Ju,Mulhern, Mathew M.,Wodka, Derek,Lynch, John K.,Engstrom, Kenneth M.,Wagaw, Seble H.,Brodjian, Sevan,Dayton, Brian,Falls, Doug H.,Bush, Eugene,Brune, Michael,Shapiro, Robin D.,Marsh, Kennan C.,Hernandez, Lisa E.,Collins, Christine A.,Kym, Philip R.
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p. 5293 - 5297
(2007/10/03)
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