【摘要】 目的:合成新型质子泵抑制剂泰妥拉唑。方法:以2,6-二氯吡啶(Ⅰ)为起始原料,经3-位硝化、2-位氨代、6-位甲氧基化、还原和环化得到5-甲氧基-2-巯基咪唑并[4,5-b]吡啶(Ⅵ),Ⅵ与2-氯甲基-4-甲氧基3,5-二甲基-吡啶缩合,经氧化得泰妥拉唑(Ⅷ)。结果:反应总收率20.9%,产物结构经1H NMR和MS确证。结论:本合成的收率与文献报道相当,是一条可行的合成泰妥拉唑。更多还原

【Abstract】 Aim:To synthesize a new proton pump inhibitor tenatoprazole.Methods:2,6-Dichloropyridine was subject to be 3-nitrified,2-ammoniated,6-substituted by sodium methoxide,then reduced and finally cycled to generate 6-methoxy-1H-benzoimidazole-2-thiol（Ⅵ）.The compound Ⅵ was condensed with 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine and then oxygenated to yield tenatoprazole.Results:The overall yield of the reaction was 20.9 %,and the structure was confirmed by（）¹H NMR and MS.Conclusion:Synthetic route and methods are feasible in the tenatoprazole preparation with the yield consistent with the reports.更多还原