A Critical Account of Synthetic Approaches toward Vildagliptin, an Antidiabetic Drug

Vildagliptin is an oral antidiabetic agent used to treat type 2 diabetes. It works by selectively inhibiting dipeptidyl peptidase IV and is preferred over other oral antidiabetic drugs due to its mechanism of action and superior gastrointestinal (GI) tolerability. In pursuit of effective treatment, Novartis AG invented vildagliptin in 1998. The drug is known under the trade names Zomelis and Galvus and was approved by the European Medicines Agency in 2008. The growing consumption of the vildagliptin active ingredient has gained much attention in the organic chemistry community; hence, inexpensive and safe manufacturing routes in environmentally benign protocols have been developed. However, there is no review article covering all synthetic processes of vildagliptin, and reviewing all of the innovative routes in one article is worthwhile.