866546-07-8Relevant articles and documents
Synthetic method of indole or azabenzopyrrole compound
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, (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.
Simple preparation method of 5-halogenated-7-azaindole
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Paragraph 0044; 0045, (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 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)
Synthesis method of 5-chloro-7-azaindole
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Paragraph 0031; 0039; 0047; 0055; 0063; 0071; 0073, (2017/08/25)
The invention provides a synthesis method of 5-chloro-7-azaindole. The synthesis method comprises the following steps: (1) reacting a dilithium initiator and trimethylbromosilane to prepare silicon-containing organic lithium; (2) reacting 2-amino-3-methylpyridine and di-tert-butyl dicarbonate to prepare 2-N-BOC-amino-3-methylpyridine; (3) performing lithiation on the 2-N-BOC-amino-3-methylpyridine through the silicon-containing organic lithium, and performing delithiation activation, cyclization and dehydration to prepare 7-azaindole; (4) performing hydrogenation reduction reaction on the 7-azaindole to generate 2,3-dihydro-7-azaindole; (5) performing chlorination reaction on the 2,3-dihydro-7-azaindole through liquid chlorine to generate 5-chloro-2,3-dihydro-7-azaindole; and (6) performing dehydrogenation reaction on the 5-chloro-2,3-dihydro-7-azaindole to obtain 5-chloro-7-azaindole. The synthesis method provided by the invention has the advantages of mild conditions and high yield.
NOVEL FURANONE DERIVATIVE
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Paragraph 0078; 0079, (2014/02/16)
To provide a novel furanone derivative, and a medicine including the same. The furanone derivative is represented by the formula (I): wherein A represents —COOR1 or a hydrogen atom; R1 represents a hydrogen atom, an optionally substituted hydrocarbon grou
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.
PROCESS FOR THE MANUFACTURE OF PHARMACEUTICALLY ACTIVE COMPOUNDS
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Page/Page column 14, (2011/02/25)
According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as novel synthesis routes for key intermediates used in those processes.
AZAINDOLES AS JANUS KINASE INHIBITORS
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Page/Page column 31, (2011/11/13)
The present invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof. Compounds of formula I are inhibitors of Janus kinases and as such are useful for the treatment of various diseases and conditions mediated by said enzym
SELECTIVE AZOLE PDE10A INHIBITOR COMPOUNDS
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, (2010/11/29)
The invention pertains to heteroaromatic compounds of the formula I, as defined herein, that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE10. The invention also relates to pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders.
COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
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Page/Page column 35, (2008/12/06)
Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
