利托那韦的制备新方法

A Novel Preparation Method of Ritonavir

建立了利托那韦的制备新方法。化合物(1)与化合物(2)在2-(7-氧化苯并三氮唑)-N,N,N',N'-四甲基脲六氟磷酸酯催化下经缩合反应合成了利托那韦,其结构经~1H NMR、^(13)C NMR、MS、元素分析和X-ray diffraction确证。在最佳反应条件[1 0.2 mol,HATU 0.2 mol,乙酸乙酯为溶剂,N-甲基吗啉为缚酸剂,于40℃反应过夜]下,收率87.4%。

A novel preparation method of ritonavir was established.Ritonavir was prepared by the reaction of compound（1） with compound（2） using 2-（7-aza-1H-benzotriazole-1-yl）-1,1,3,3-tetramethyluronium hexafluoropho sphate as the catalyst and N-methylmorpholine as the acid-binding agent.The product structure was confirmed by ~1H NMR,^（13）C NMR,MS,elemental analysis and X-ray diffraction. Under the optimum reaction conditions [compound（1）0.2 mol, HATU 0.2 mol, ethyl acetate as the solvent,N-methylmorpholine as the acid-binding agent,at 40℃ for one night ], the yield can reach to 87.4%.