183208-35-7Relevant articles and documents
Full functionalization of the 7-azaindole scaffold by selective metalation and sulfoxide/magnesium exchange
Barl, Nadja M.,Sansiaume-Dagousset, Elodie,Karaghiosoff, Konstantin,Knochel, Paul
, p. 10093 - 10096 (2013)
Filling positions: 7-Azaindoles are important targets in the pharmaceutical industry. All five carbon positions of the azaindole ring system can be functionalized in a predictable manner starting from the appropriately substituted azaindole 1 by directed metalation and halogen/magnesium and sulfoxide/magnesium exchange. The products are fully substituted azaindoles of type 2.
Simple preparation method of 5-halogenated-7-azaindole
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Paragraph 0046-0049, (2019/10/01)
The invention discloses a simple preparation method of 5-halogenated-7-azaindole. The method comprises: carrying out a 1,4-addition reaction on 4,4-dialkoxy n-butyronitrile (II) and 2,3-dihalogenatedacrolein (III) in the presence of a solvent and a catalyst to generate 2,3-dihalogenated-4-cyano-6,6-dialkoxy n-hexanal (IV), and carrying out a cyclization reaction on the 2,3-dihalogenated-4-cyano-6,6-dialkoxy n-hexanal, an alkali, ammonia and an ammonium salt to prepare the 5-halogenated-7-azaindole (I). According to the present invention, the method has characteristics of inexpensive and easily available raw materials, short process route, less wastewater discharge, easy environmental protection, convenient reaction operation, high reaction selectivity, high product purity, high yield andlow cost, and is suitable for the environmentally-friendly industrial production of 5-halogenated-7-azaindole.
A medicine intermediate 5 - bromo -7 - aza indole synthesis method
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Paragraph 0022; 0028; 0031; 0034; 0035; 0040; 0046, (2019/03/28)
The present invention discloses a pharmaceutical intermediate 5 - bromo - 7 - aza indole synthesis method, comprises the following steps: to 2 - nitro - 3 - methyl - 5 - bromo pyridine as raw materials, and DMA and DMF mixture prepared by the reaction of 2 - nitro - 3 - dimethylamine vinyl - 5 - bromo pyridine, after the reaction with the aniline - sodium, to obtain 5 - bromo - 7 - azaindole. The application of the synthesis method is simple in operation, mild condition, less by-products, the product has high purity, product yield is relatively high.