CHAPTER 5: Question 6

 

Simple Answers


The initial reaction is a straight forward resolution in which the salt of the (S)-enantiomer of the amino ester and the (R,R)-isomer of the tartaric acid derivative has a low solubility in water and so crystallizes from the solution. The diastereomeric salt formed from the (R)-enantiomer of the amino ester and the (R,R)-dibenzoyl tartrate is more soluble in water and so does not precipitate from the reaction mixture. The addition of benzaldehyde to the resulting solution (which will mostly consist of the (R)-enantiomer of the amino ester) reversibly forms an imine with the amino group of the amino ester. This increases the acidity of the hydrogen atom attached to the stereocentre to such an extent that rapid racemization occurs under the reaction conditions. This forms more of the (S)-enantiomer of the amino ester which again precipitates from solution. It is theoretically possible for this process to give a 100% yield of the (S)-enantiomer of the amino ester complexed to (R,R)-dibenzoyl tartrate, but in practice a 70% yield of the salt is obtained.

This example is taken from: J.D. Moseley, B.J. Williams, S.N. Owen, and H.M. Verrier; Tetrahedron: Asymmetry, 1996, 7, 3351-2.
 

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