CONTROLLED DESIGN OF RESOLUTIONS - PREDICTION OF THE EFFICIENCY OF RESOLUTIONS BASED ON SAMPLES OF ARBITRARY COMPOSITION

The rational design of resolution processes is a topic of common inter est for the industrial synthesis of enantiopure compounds. However, no efficient method for selecting suitable resolving agents for classica l resolution using diastereomeric salts is available yet(1) and the se lection of an appropriate resolving agent usually is a matter of trial and error. This article describes an approach using single differenti al scanning calorimetry (DSC) measurements on mixtures of diastereomer s with arbitrary (non-racemic) compositions, with the aim of allowing a more systematic identification of efficient resolving agents and to minimize the possible errors due to uncontrolled experimental factors in the search for resolving agents. It is shown that in many cases a s ingle DSC thermogram can provide valuable information about the maxima l possible efficiency of an enantiomer resolution via diastereomeric s alts. (C) 1998 Elsevier Science Ltd. All rights reserved.