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【结 构 式】

【药物名称】EF-4040, ME-3407

【化学名称】2-(Butoxycarbonylmethylsulfinyl)thiazolo[5,4-b]pyridine
      2-(Thiazolo[5,4-b]pyridin-2-ylsulfinyl)acetic acid butyl ester

【CA登记号】133903-90-9

【 分 子 式 】C12H14N2O3S2

【 分 子 量 】298.38498

【开发单位】Meiji Seika (Originator)

【药理作用】Antiulcer Drugs, Gastric Antisecretory Drugs, GASTROINTESTINAL DRUGS

合成路线1

2-Mercaptothiazolo[5,4-b]pyridine (I) is treated with chloroacetic acid butyl ester (II) in the presence of potassium carbonate in DMF to give 2-[(butoxycarbonylmethyl)thio]thiazolo[5,4-b]pyridine (III), which is oxidized with m-chloroperbenzoic acid in dichloromethane.

1 Katano, K.; Tomomoto, T.; Ogino, H.; Yamazaki, N.; Hirano, F.; Yuda, Y.; Konno, F.; Nishio, M.; Machinami, T.; Shibahara, S.; Tsuruoka, T.; Inouye, S. (Meiji Seika Kaisha, Ltd.); Azole derivs. and antiulcerative compsn. containing same. EP 0405976; JP 1991218377; US 5079255; US 5141946; US 5200407 .
2 Castaner, J.; Mealy, N.; Prous, J.; ME-3407. Drugs Fut 1994, 19, 1, 31.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 14594 [1,3]thiazolo[5,4-b]pyridine-2-thiol; [1,3]thiazolo[5,4-b]pyridin-2-ylhydrosulfide C6H4N2S2 详情 详情
(II) 14595 n-Butyl Chloroacetate; butyl 2-chloroacetate 590-02-3 C6H11ClO2 详情 详情
(III) 14596 butyl 2-([1,3]thiazolo[5,4-b]pyridin-2-ylsulfanyl)acetate C12H14N2O2S2 详情 详情
Extended Information