| 摘要 |
Disclosed is a method for producing aminocarbonyl compounds of the general formula (I) wherein R1 and R2 can be identical or different and represents hydrogen, alkyl, alkenyl, alkynyl, or aryl, X represents hydrogen, alkyl, alkenyl, alkynyl, aryl, or OR3, R3 representing hydrogen, alkyl, alkenyl, alkynyl, or aryl. According to said method, an aldehyde of the general formula (II) R1CO (II) wherein R1 has the meaning indicated above, is reacted with an imine of the general formula (III) wherein R2 and X have the meaning indicated above, in the presence of a catalyst. Aminocarbonyles are obtained by means of catalyzed Mannich reactions with aldehydes. For example, if alpha-unbranched aldehydes are reacted with previously formed N-Boc imines in the presence of (S)-proline as a catalyst, the desired beta-amino aldehydes are obtained at excellent yields, diastereoselectivities and enantioselectivities.
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