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Patent / Nov 13, 2008

Methods and intermediates for synthesis of selective dpp-iv inhibitors

  • Emilia Leitao
  • David Alan Campbell
  • Zhen-Ping Wu
  • Peng Wang

Methods and intermediates for the synthesis of selective inhibitors of dipeptidyl peptidase IV (DPP-IV) are provided. Coupling of a carboxylate salt with a boro-proline derivative provides a protected form of a DPP-IV inhibitor, which may be deblocked to yield the medicinal compound. The carboxylate salt can be a crystalline form of a sodium salt or a dicyclohexylammonium salt. The inhibitor can be used in the treatment of diabetes.