Direct Synthesis of Cyanopyrrolidinyl [beta]-Amino Alcohols for the Development of Diabetes Therapeutics

Cyanopyrrolidinyl [beta]-amino alcohols are novel scaffolds with potential for a wide array of pharmacological properties. We have discovered that we can selectively access these scaffolds from simple and inexpensive commercially available chemicals in few synthetic steps with minimal purification. We have produced a 36-compound library of these scaffolds and tested them as dipeptidyl peptidase IV (DPP4) inhibitors. These novel inhibitors are useful in the treatment of diabetes and inflammatory disorders.