851086-95-8Relevant articles and documents
A chiral three-stage amine compound synthetic methods and use thereof
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Paragraph 0030; 0033; 0034, (2019/05/21)
The present invention provides a chiral three-stage compound synthesis method, the method is asymmetric reductive amination reaction, the use of two-stage [...] iridium catalyst in the hydrogenation reaction under the action of the chiral three levels of amine compounds, the method of preparation and chiral three levels of amine compounds can be used for anti-depression drugs and the like synthetic. The relates to chiral three-stage amides synthetic method, the secondary amine as asymmetric reductive amination of amine source, and not through the other chemical reactions by one step to obtain three levels of chiral amine; the use of phosphoramidite chiral ligand as catalyst, such chiral ligand low price, easy synthesis and expand; additive combined use can greatly improve the yield of the reaction and the enantioselectivity. From the foregoing, the method has simple operation and easy mass production advantages.
IMPROVED PROCESS FOR THE PREPARATION OF RIVASTIGMINE
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Page/Page column 9, (2008/06/13)
The present invention relates to an improved process for preparation of Rivastigmine of formula (I) or pharmaceutically acceptable salts thereof comprising a step of N-methylation of compound of formula (III), wherein R1 = R2 = H or R1 = H and R2 = CH3 or an acid addition salt thereof, using paraformaldehyde in the presence of Raney Nickel and hydrogen in a suitable solvent to obtain compound of formula (II).
