- Method for preparing 5-hydroxy-7-azaindole
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The invention discloses a method for preparing 5-hydroxy-7-azaindole. The intermediate structure is shown in the formula III. The method comprises that a compound 5-bromo-7-azaindole shown in the formula I as a raw material undergoes a nitrogen protection reaction and a hydroxylation and direct deprotection reaction to produce 5-hydroxy-7-azaindole shown in the formula III. The method utilizes cheap and easily available raw materials, realizes a low cost, is used under mild reaction conditions, has a high yield and is suitable for industrial large-scale production.
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Paragraph 0063-0066; 0084-0089; 0109-0112
(2017/12/28)
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- Rapid preparation of triazolyl substituted NH-heterocyclic kinase inhibitors via one-pot Sonogashira coupling-TMS-deprotection-CuAAC sequence
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The one-pot, three-component Sonogashira coupling-TMS-deprotection-CuAAC ("click") sequence is the key reaction for the rapid synthesis of triazolyl substituted N-Boc protected NH-heterocycles, such as indole, indazole, 4-, 5-, 6-, and 7-azaindoles, 4,7-diazaindole, 7-deazapurines, pyrrole, pyrazole, and imidazole. Subsequently, the protective group was readily removed to give the corresponding triazolyl derivatives of these tremendously important NH-heterocycles. All compounds have been tested in a broad panel of kinase assays. Several compounds, 8f, 8h, 8k, and 8l, have been shown to inhibit the kinase PDK1, a target with high oncology relevance, and thus they are promising lead structures for the development of more active derivatives. The X-ray structure analysis of compound 8f in complex with PDK1 has revealed the detailed binding mode of the molecule in the kinase. The Royal Society of Chemistry 2011.
- Merkul, Eugen,Klukas, Fabian,Dorsch, Dieter,Graedler, Ulrich,Greiner, Hartmut E.,Mueller, Thomas J. J.
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supporting information; experimental part
p. 5129 - 5136
(2011/09/13)
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