Loops Patents (Class 54/87)
  • Patent number: 6774236
    Abstract: The invention relates to a process and intermediates for the preparation of enantiomerically pure cycloalkanoindolecarboxylic acids and azaindolecarboxylic acids and pyrimido[1,2a]indolecarboxylic acids and their activated derivatives, characterized in that the tolyl acetic acid is first esterified with a chiral alcohol, then diastereoselective substitution at &agr;-carbon atoms is carried out and this product is halogenated in the tolyl group and then reacted with appropriate cycloalkanoindoles, cycloalkanoazaindoles or pyrimido[1,2a]indoles. It is possible by this method to prepare specifically, in high purity, the enantiomerically pure carboxylic acids which are intermediates for valuable medicaments.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: August 10, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Jan-Bernd Lenfers, Peter Fey, Paul Naab, Kai Van Laak