866546-07-8Relevant articles and documents
Synthetic method of indole or azabenzopyrrole compound
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Paragraph 0114-0118, (2021/03/31)
The invention relates to a synthetic method of an indole or azabenzopyrrole compound. The synthetic method comprises the following steps: carrying out cyclization reaction on a compound A and disubstituted amine in a solvent, wherein the structural general formula of the disubstituted amine is NH(R2)2, R2 is respectively and independently selected from C1-C6 alkyl, C1-C6 alkyl hydroxyl, C1-C6 alkyl O-C1-C6 alkyl, C1-C6 alkyl NH-C1-C6 alkyl or C1-C6 alkylamino, and the two R2 are connected with each other to form a ring or not form a ring. According to the synthetic method of the indole or azabenzopyrrole compound, the disubstituted amine compound with a specific structural general formula and the terminal alkynyl of the intermediate are subjected to an addition reaction, the rigid structure of the terminal alkynyl is changed, and the structure of alkenyl amine is changed, so that under mild reaction conditions, ring closing of pyrrole groups in indole or azabenzopyrrole compounds is realized, side reactions are few, the product yield is high, and the production cost of the product is reduced from the source.
A 5 - chloro -7 - aza indole synthesis method (by machine translation)
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Paragraph 0031; 0032; 0037-0044; 0047; 0048; 0055; 0056, (2018/06/26)
The invention discloses a 5 - chloro - 7 - aza indole synthesis method, comprises the following steps: to the 7 - aza indole to carry out chlorination reaction for the preparation of 5 - chloro - 7 - aza-indoline, the obtained 5 - chloro - 7 - aza-indoline with toluene mixed added in a reaction kettle, heating to 40 - 60 °C, after adding catalyst, is irradiated by microwave in 60 - 90 min, stirring reaction after 1 - 2 h, after the reaction, filtration, the filtrate is distilled under reduced pressure to remove the toluene, recrystallized 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. (by machine translation)
The acid-catalysed synthesis of 7-azaindoles from 3-alkynyl-2- aminopyridines and their antimicrobial activity
Leboho, Tlabo C.,Van Vuuren, Sandy F.,Michael, Joseph P.,De Koning, Charles B.
, p. 307 - 315 (2014/01/06)
The synthesis of 7-azaindoles from 3-alkynyl-2-aminopyridines using acidic conditions, namely, a mixture of trifluoroacetic acid (TFA) and trifluoroacetic anhydride (TFAA), is described. This methodology resulted in the synthesis of fifteen 7-azaindoles, with most containing substituents at the 2- and 5-positions. The majority of these were tested for antimicrobial activity against a range of bacteria and yeasts. The 7-azaindoles displayed the best activity against the yeasts, particularly against Cryptococcus neoformans, where activities as low as 3.9 μg ml-1 were observed.
