- Applicability aspects of transition metal-catalyzed aromatic amination protocols in medicinal chemistry
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The application of palladium- and coppercatalyzed reactions for the aromatic amination of pharmacologically relevant scaffolds is investigated. The focus is set on the scope of several protocols for the introduction of amines of broad structural diversity, allowing for the synthesis of numerous derivatives of one biological hit structure for screening in biological assay systems. Thus, attaining optimized yields and TONs had not a major priority, most important were practical aspects, that is no further purification and drying of reagents and solvents had to be envisaged, ideally only a few transition metalbased protocols had to be applied for synthesizing structurally diverse compounds in sufficient amounts (several milligrams) for screening without any finetuning of conditions and catalytic systems.
- Tasler, Stefan,Mies, Jan,Lang, Martin
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p. 2286 - 2300
(2008/09/19)
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- A Convenient One-Pot Preparation of Bis(nitroaryl) Tellurides Using a Tellurium-Copper Couple as the Telluration Reagent
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The Te-Cu couple generated in situ by the reaction of disodium telluride with copper(I) iodide in dry N-methyl-2-pyrrolidone has been found to be a convenient telluration reagent for some activated iodoarenes 1.Using this reagent system, we have prepared
- Suzuki, Hitomi,Nakamura, Tohru
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p. 783 - 786
(2007/10/02)
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