19230-57-0Relevant articles and documents
A Journey through Hemetsberger–Knittel, Leimgruber–Batcho and Bartoli Reactions: Access to Several Hydroxy 5- and 6-Azaindoles
Radix, Sylvie,Hallé, Fran?ois,Mahiout, Zahia,Teissonnière, Amélie,Bouchez, Grégoire,Auberger, Ludovic,Barret, Roland,Lomberget, Thierry
, (2022/02/22)
The preparation of various 5- and 6-azaindoles, heterocyclic structures that are frequently part of molecules in clinical development, and their monohydroxy analogues were described. Different strategies, relying on the de novo pyrrole ring formation, were investigated and, thanks to Hemetsberger–Knittel, Bartoli and Leimgruber–Batcho approaches, 4- and 7-monohydroxy 5- and 6-azaindoles were obtained. The crucial introduction of the oxygen atom was carried out from halogen derivatives, using nucleophilic substitution reactions under basic conditions with or without a copper catalyst. Some preliminary oxidation reactions have shown that it was yet not possible to synthesize the azaquinone indole structure from monohydroxy azaindole, using molecular oxygen in the presence of salcomine as a catalyst.
Technological method for preparing 2- amino -6-5-methyl-substituted-pyridine (by machine translation)
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Paragraph 0055-0057, (2020/01/12)
The reaction solvent of 2 - the method is reacted in a reaction solvent under the action, of 2 - an, acid anhydride and an acid,binding, agent and an amination reagent under the action. of an acid anhydride and 2 - an acid-binding agent and, an amination reagent, 2 -4 - 93/7, 99.8%, 70%. (by machine translation)
PROCESS FOR PREPARATION OF LUMACAFTOR
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Paragraph 0164, (2017/05/07)
The present invention relates to a process for the preparation of amorphous lumacaftor. The present invention relates to a process for the preparation of intermediate 6-amino-2- halo-3-methylpyridine compounds used in the preparation of lumacaftor. The present invention relates to lumacaftor hydrobromide, process for its preparation and conversion thereof to lumacaftor.