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目的研究莫扎伐普坦的合成工艺。方法以邻氨基苯甲酸甲酯为起始原料,经N-磺酰化、烃化、环合、脱羧、N-甲基化、还原胺化等反应制得关键中间体8;以对氨基苯甲酸甲酯为原料,经N-酰化、酯水解和酰氯化制得另一中间体11;8与11于丙酮中反应制得目标化合物。结果与结论目标化合物的结构经1H-NMR、M S等确证。总收率达14.2%(以邻氨基苯甲酸甲酯计)。该路线操作简便,条件温和,有利于工业应用。
Objective To study the synthesis of movafaiptan. Methods Starting from methyl anthranilate, the key intermediate 8 was prepared by N-sulfonylation, alkylation, cyclization, decarboxylation, N-methylation and reductive amination. Methyl formate as starting material, N-acylation, ester hydrolysis and acid chloride to prepare another intermediate 11; 8 and 11 in acetone to obtain the target compound. Results and Conclusions The structures of the target compounds were confirmed by 1H-NMR, MS and so on. The total yield of 14.2% (with methyl anthranilate). The route is easy to operate, mild conditions, is conducive to industrial applications.