Synthesis method of lisethopram and intermediate of lisethopram

Abstract

The invention provides a synthesis method of lisethopram and an intermediate thereof, and the synthesis method of lisethopram comprises the following steps: ingeniously utilizing the activity difference of reactive groups to carry out regioselective coupling reaction on a compound shown as a formula I and a compound shown as a formula II, and carrying out buchwald coupling reaction on a generated compound shown as a formula III and a compound shown as a formula IV to obtain lisethopram or a derivative thereof. In the synthesis method, the yield and the purity of an intermediate compound shown as a formula III obtained in the first step of reaction are high, an expensive intermediate compound shown as a formula IV is introduced in the following steps, the production cost is greatly reduced, the synthesis method is suitable for industrial production, and the problem of low yield of nucleophilic substitution reaction in the original research process is also solved by the buchwald reaction in the second step of reaction; the final product lisethopram obtained by the synthesis method is high in purity and high in yield. # imgabs0 #

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