Beilstein J. Org. Chem.2008,4, No. 20, doi:10.3762/bjoc.4.20
-cells [1].
Because of its key role in DPP-IV inhibition the 2(S)-cyanopyrrolidine moiety has been found to be an integral part of many DPP-IV inhibitors (Figure 1). Apart from behaving as a proline mimic, the presence of the nitrile on the five-memberedring provides (i) reversible and nanomolar
Beilstein J. Org. Chem.2007,3, No. 35, doi:10.1186/1860-5397-3-35
under solvent-free conditions affording acyl benzothiophenes in good overall yields.
Background
Benzothiophene derivatives possessing an acyl group as one of the substituents on the five-memberedring are of immense medicinal value because of their promising pharmacological properties. For example
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Graphical Abstract
Figure 1:
Acyl benzothiophenes of pharmacological interest.