Patent ID: 6187582
Filing Date: 2001-02-13
Classification: C07C,C12P,G01K

Abstract:
A process for preparing an optically active amine of the formula ##STR28##whereinR represents a radical of the formula--(CH.sub.2).sub.m --R.sup.2, andR.sup.2 represents optionally substituted phenyl of the formula ##STR29##whereinR.sup.7, R.sup.8 and R.sup.9 independently of one another each represent hydrogen, halogen, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, alkylthio having 1 to 4 carbon atoms, halogenoalkyl having 1 to 4 carbon atoms and 1 to 5 identical or different halogen atoms, halogenoalkoxy having 1 to 4 carbon atoms and I to 5 identical or different halogen atoms, cyano, dialkylamino having 1 to 4 carbon atoms in each alkyl group, nitro, phenyl, phenoxy or benzyl, andm represents the numbers 0, 1, 2 or 3, andR.sup.1 represents hydrogen, comprising the steps ofa) reacting in a first step, a racemic amine of the formula ##STR30##whereinR and R.sup.1 are each as defined above with an ester of the formula ##STR31##whereinR.sup.3 represents chloromethyl or a radical of the formula --CH.sub.2 --CN, orR.sup.3 represents a radical of the formula --CH.sub.2 --COOR.sup.6, whereinR.sup.6 represents methyl, ethyl, n-propyl or n-butyl, andR.sup.4 represents methyl, ethyl, n-propyl, or n-butyl, in the presence of lipase from Candida antarctica and in the presence of a diluent,b) separating, in a second step, the resulting mixture of (S)-amine of the formula ##STR32##whereinR and R.sup.1 are each as defined above, and separating the acylated (R)-amine of the formula ##STR33##whereinR, R.sup.1 and R.sup.3 are each as defined above, andc) if appropriate, setting free, in a third step, the (R)-amine of the formula ##STR34##whereinR and R.sup.1 are each as defined above, from the acylated (R)-amine of the formula (III) by treatment with an acid or a base, if appropriate in the presence of a diluent.