NOVEL METHOD FOR THE PREPARATION OF (S)-PREGABALIN

    公开(公告)号:WO2011076915A8

    公开(公告)日:2011-06-30

    申请号:PCT/EP2010/070634

    申请日:2010-12-23

    Abstract: Method for the preparation of a salt (III) of pregabalin and (S)-mandelic acid with a (S, S) diastereomer content greater than 80% which comprises the following steps: (a) Hofmann reaction of (±)-3-(carbamoylmethyl)-5- methylhexanoic acid (I) to obtain racemic pregabalin (II), (b) addition of (S)-(+)-mandelic acid to obtain the corresponding diastereoisomeric salt (III) with a (S, S) diastereomer content greater than 80% (c)optionally, purification of the salt obtained in step (b); characterized in that step(b) is performed without isolating the product obtained in step(a).

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