Total synthesis and biological evaluation of fluoroolefin-containing dipeptide isosteres as inhibitors of dipeptidyl peptidase IV (CD26)

The total synthesis and the biological evaluation of fluoroolefin-containing (Z)-N-peptidyl-O-hydroxylamine dipeptide isosteres, 1 and 2, are described in this work. The synthetic strategy relies on the efficient construction of the fluoroolefin moiety by a modified Peterson olefination reaction employing tert-butyl...