Stereochemical switch driven by crystallization: Interplay between stoichiometry and configuration of the products

Chirality. 2022 Jul;34(7):948-954. doi: 10.1002/chir.23451. Epub 2022 Apr 26.

Abstract

An intriguing example of a crystallization-induced stereochemical switch in the configuration of aza-Michael reaction products is described. Depending on both the stereochemical purity and stoichiometric ratio of the chiral amine used, the reaction delivers crystalline diastereomers of a different stereochemistry. The optically pure diastereomer smoothly converts to its racemic epimer salt upon the addition of a complementary chiral amine.

Keywords: amino acid; aza-Michael addition; crystallization-induced diastereomer transformation; dynamic covalent chemistry; homophenylalanine; indanone; isomerization.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amines*
  • Crystallization
  • Stereoisomerism

Substances

  • Amines