API Case Study: Praziquantel

Cao et al. have developed a route incorporating a multicomponent reaction for the synthesis of Praziquantel, a drug on the WHO list of essential medicines used for the treatment of schistosomiasis.[1] An Ugi four component reaction is first applied to produce an acylated intermediate which is subsequently cyclised via a Pictet-Spengler reaction. This has been demonstrated on a small scale and this route shows promise as a mass efficient two-step synthesis of Praziquantel. Additional benefits are that the by-products from the two steps are water and two equivalents of methanol and the reaction conditions are mild.