1240038-86-1Relevant articles and documents
Preparation method of 3R-amino substituted butyrylamide derivative
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Paragraph 0080; 0081, (2016/10/09)
The invention relates to a preparation method of a 3R-amino substituted butyrylamide derivative. The preparation method of the 3R-amino substituted butyrylamide derivative comprises the following steps: carrying out hydrogenation reduction on enamine II for preparing 3R,3S-amino substituted butyrylamide racemate III; carrying out resolution, and filtering, so as to obtain 3R-amino substituted butyrylamide R(-) mandelate with high ee% value, alkalifying to obtain the 3R-amino substituted butyrylamide derivative; and oxidizing the obtained mother liquor, so as to obtain enamine II in a recycling manner, and repeating oxidation-reduction cycle for multiple times until products at specified yield are obtained. The preparation method of the 3R-amino substituted butyrylamide derivative has the advantages that a cyclic method is utilized for converting 3S-amino substituted butyrylamide racemate or 3R,3S-amino substituted butyrylamide mixture in any ratio into the 3R-amino substituted butyrylamide derivative with high ee% value, so that the mother liquor is effectively utilized; meanwhile, an expensive catalyst or asymmetric reductive amination with high demand condition does not need to be adopted, thereby being beneficial to reduction of cost and clean production.
