- Preparation method for 4,6-dichloroindole
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The invention discloses a preparation method for 4,6-dichloroindole. The preparation method comprises the following specific steps: in an acidic condition of 3,5-dichloroaniline, carrying out a diazo-reaction on sodium nitrite and then carrying out a condensation reaction with ethyl pyruvate to obtain ethyl-2-(2-(3,5-dichlorophenyl) hydrazono) propionic acid; carrying out ring formation on the ethyl-2-(2-(3,5-dichlorophenyl) hydrazono) propionic acid under the action of lewis acid to obtain 4,6-dichlorindole ethyl formate; hydrolyzing the 4,6-dichlorindole ethyl formate under action of lithium hydroxide to obtain 4,6-dichloroindolecarboxylic acid; and carrying out decarboxylation on the 4,6-dichloroindolecarboxylic acid to obtain 4,6-dichloroindole. The synthetic process of the inventionis more economic, environmentally friendly, efficient and simple.
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Paragraph 0046-0048; 0049-0051; 0052-0054
(2019/01/17)
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- Continuous-flow synthesis of monoarylated acetaldehydes using aryldiazonium salts
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Anilines and ethyl vinyl ether can be used as precursors for a process that is the synthetic equivalent of the α-arylation of acetaldehyde enolate. The reaction manifests a high level of functional group compatibility, allowing the ready preparation of a number of synthetically valuable compounds.
- Chernyak, Natalia,Buchwald, Stephen L.
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supporting information; experimental part
p. 12466 - 12469
(2012/09/05)
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- NMDA ANTAGONISTS
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The present invention is directed to a class of 4,6-disubstituted tryptophan derivatives, 4,6-disubstituted kynurenines, their use as NMDA antagonists and to pharmaceutical compositions containing these compounds.
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