Examples of Enantioseparations in the Pharmaceutical Industry

The deficient amount of the acid was supplemented by HCl. Yield is based on a half amount of the racemate. Enantiomeric excess is of the recovered amine. 

Similar enantioseparation processes applying the solvent switch have been reported for the enantioseparation of racemic l-phenyl-2-(4-methylphenyl)ethyl-amine and 2-(4-methoxyphenyl)-3-acetoxy-5-(2-(dimethylamino)ethyl)-2,3-dihydro-l,5-benzothiazepin-4(5H)-one with enantiopure mandelic acid [34]. 

It has been estimated that more than a half of chiral drugs in pharmaceutical mar- 

150 I 5 Resolution of Chiral Drugs and Drug Intermediates by Crystallisation 

MeOH 8(v/wt) Molar ratio 0.7 Yield 96% Enantiomeric excess 99% 

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Examples of Enantioseparations in the Pharmaceutical Industry 149 Table 5.13 Enantioseparation of la-amino- -caprolactam with N-tosyl-t-phenylalanine. 

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