120739-84-6Relevant articles and documents
Selective N -monomethylation of primary anilines with the controllable installation of N -CH2D, N -CHD2, and N -CD3units
Meng, Jing,Wang, Yi-Feng,Wang, Zhijuan,Xia, Hui-Min,Xu, Ai-Qing,Zhang, Feng-Lian
, p. 4922 - 4926 (2020)
The selective N-monomethylation of primary anilines was realized by the use of the Me3N-BH3/N,N-dimethylformamide (DMF) system as the methyl source. This method also allows for the controllable introduction of N-CH2D, N-CHD2, and N-CD3 units with high lev
Method for preparing netupitant
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Paragraph 0047; 0050-0051, (2018/04/02)
The invention discloses a method for preparing netupitant, and belongs to the field of medicine compounds. The method includes the steps: performing condensation on 2-chloro-5-aminopyridine and formicacid; performing reduction, Boc protection and iodination; performing coupling and deprotection and then performing condensation on products and 2-(3, 5-bis-trifluoromethyl-phenyl)-2-methyl propionicacid; performing substitution on products and N-methylpiperazine to obtain the netupitant. The method has the advantages that the steps of processes for preparing the netupitant have fewer side effects, the method is high in yield and less in environmental pollution, after-treatment is simple, and the netupitant which is a product prepared by the aid of the method is high in purity and low in individual impurity content.
Ortho-hydroxyalkylation of aminopyridines: A novel approach to heterocycles
Zakrzewski, Peter,Gowan, Mathew,Trimble, Laird A.,Lau, Cheuk K.
, p. 1893 - 1902 (2007/10/03)
Reaction of 6-substituted N-alkyl-3-aminopyridines with aldehydes in the presence of dichlorophenylborane gives selectively 2-hydroxyalkyl-3- aminopyridines. Dehydration of the latter under pyrolytic or Lewis acid conditions generates a quinone methide imine intermediate which can undergo electrocyclic or [4+2] cycloaddition reactions to give naphthyridines, dihydronaphthyridines or tetrahydronaphthyridines. Palladium-catalyzed cyclization of the 2-(1-hydroxyallyl)-3-aminopyridines gives the corresponding 4-azaindoles.