Improved Synthesis Of Landiolol Hydrochloride

Objective: To study on synthesis of landiolol;Methods: Ethylenediamine,as the starting material,was selectiveprotected by using di-tert-butyl carbonate, then reacted with the productwhich produced by morpholine and N,N’-carbonyldiimidazoltotert-butyl(2-(morpholine-4-carboxamido)ethyl)carbamate. Then de-Bocproduct and purified by the acidification and basification using oxalate andNaOH to N-(2-aminoethyl)morpholine-4-carboxamide,which reacted with(S)-(2,2-dimethyl-1,3-dioxolan-4-yl)methyl3-(4-(cyclopropylmethoxy)phenyl)propanoatepropionate to the target product.Results: The target compounds was successful synthesis with highpurity, structure was confirmed by1H NMR and mass spectrum, the sevenstep reaction yield was40%;Conclusion: This method has potential in industrial production.