(4-Cyclopropanesulfonyl-6-methyl-3-nitro-2-oxo-2H-pyridin-1-yl)-acetic acid ethyl ester | 210704-85-1

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: (4-Cyclopropanesulfonyl-6-methyl-3-nitro-2-oxo-2H-pyridin-1-yl)-acetic acid ethyl ester
• CAS: 210704-85-1
• 化学式: C₁₃H₁₆N₂O₇S
• 分子量: 344.345
• InChiKey: XNLFHGDHHPJJLU-UHFFFAOYSA-N

反应信息

• 作为反应物：
  描述：

  (4-Cyclopropanesulfonyl-6-methyl-3-nitro-2-oxo-2H-pyridin-1-yl)-acetic acid ethyl ester 在 palladium on activated charcoal lithium hydroxide 、 氢气 作用下， 以 四氢呋喃 、 甲醇 、 乙醇 为溶剂， 生成 (3-Amino-4-cyclopropanesulfonyl-6-methyl-2-oxo-2H-pyridin-1-yl)-acetic acid
  参考文献：
  名称：

  3-Amino-4-sulfonylpyridinone acetamide and related pyridothiadiazine thrombin inhibitors

  摘要：

  We describe a series of highly potent and efficacious thrombin inhibitors based on a 3-amino-4-sulfonylpyridinone acetamide template. The functionally dense sulfonyl group stabilizes the aminopyridinone, conformationally constrains the 4-substituent, and forms a hydrogen bond to the insertion loop tyrosine OH. We also describe a related series of fused bicyclic dihydrothiadiazinedioxide derivatives, of which one had improved pharmacokinetics in dogs after oral dosing. (C) 2003 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(03)00154-9
• 作为产物：
  描述：

  2-Cyclopropanesulfonyl-benzothiazole 、 4-chloro-1-ethyloxycarbonylmethyl-6-methyl-3-nitro-2-pyridinone 在 sodium tetrahydroborate 、 溶剂黄146 作用下， 以 乙醇 为溶剂， 生成 (4-Cyclopropanesulfonyl-6-methyl-3-nitro-2-oxo-2H-pyridin-1-yl)-acetic acid ethyl ester
  参考文献：
  名称：

  3-Amino-4-sulfonylpyridinone acetamide and related pyridothiadiazine thrombin inhibitors

  摘要：

  We describe a series of highly potent and efficacious thrombin inhibitors based on a 3-amino-4-sulfonylpyridinone acetamide template. The functionally dense sulfonyl group stabilizes the aminopyridinone, conformationally constrains the 4-substituent, and forms a hydrogen bond to the insertion loop tyrosine OH. We also describe a related series of fused bicyclic dihydrothiadiazinedioxide derivatives, of which one had improved pharmacokinetics in dogs after oral dosing. (C) 2003 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(03)00154-9