泰妥拉唑的合成  

Synthesis of tenatoprazole

作　　者：王德才[1] 胡晓曦[1] 周勤[2] 

机构地区：[1]南京工业大学制药与生命科学学院,南京210009 [2]江苏吴中苏药医药开发有限责任公司,南京210009

出　　处：《中国药科大学学报》2006年第3期284-285,共2页Journal of China Pharmaceutical University

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。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-lH-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 ^1 H NMR and MS. Conclusion： Synthetic route and methods are feasible in the tenatoprazole preparation with the yield consistent with the reports.

关 键 词：泰妥拉唑 H^+/K^+-ATP酶抑制剂 质子泵抑制剂 合成 

分 类 号：TQ463.53[化学工程—制药化工]