171596-36-4

• 常用中文名：去甲基他达那非
• 常用英文名：Nortadalafil
• CAS号：171596-36-4
• 分子式：C₂₁H₁₇N₃O₄
• 分子量：375.377
• 相关类别： 信号通路 代谢酶/蛋白酶 磷酸二酯酶(PDE)
• 发布时间：2017-12-27 13:54:16
• 更新时间：2026-07-02 14:03:02
• Nortadalafil是demethyl Tadalafil,为PDE5抑制剂。

名称

• 中文名: 去甲基他达那非
• 英文名: Nortadalafil
• 中文别名: N-去甲基他达拉非; 去甲他达那非; 他达那非杂质21; (6R,12-6-(苯并[D][1,3]二氧杂环戊烯-5-基)-2,3,6,7,12,12A-六氢吡嗪并[1',2':1,6]吡啶并[3,4-B]吲哚-1,4-二酮; 去甲他达拉非; 去甲基他达拉非杂质; 去甲基他达拉非检测标准品; 去甲基他达那非,10 MM DMSO 溶液; 去甲基他达那非 标准品; 诺塔达拉非; N-去甲基他达那非; (2R)-2-(2-氯乙酰氨基)-3-(1-(2-氯乙酰基)吲哚-3-基)丙酸甲酯(他达拉非杂质); 去甲基他达拉非溶液, 100PPM; 非他达拉非; 诺他达拉非; 甲醇中去甲基他达拉非溶液,100ΜG/ML; 去甲基他达拉非; 他达那非氮去甲基杂质; N去甲基他达拉菲; 他达拉非杂质J; N-脱甲基他达拉非; 他达拉非杂质21(N-去甲基他达拉非); 甲醇中去甲基他达拉非
• 英文别名: N-demethyltadalafil; Tadanafil N-desmethyl impurity; (6R,12aR)-6-(1,3-Benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione; Demethyltadalafil impurity; Nortadalafil, 10 mM in DMSO; N-Desmethyl tadalafil in methanol; Nortadalafil/Demethyl Tadalafil; (6R,12-6-(1,3-Benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione, N-DesMethyl Tadalafil; Tadalafil Impurity 21; Pyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione, 6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-, (6R,12); N-Desmethyl Tadalafil; Tadalafil IMpurity:IMpurity C; Tadalafil Impurity 21(N-Desmethyl Tadalafil); DeMethyltadalafil; Tadalafil IMpurity J; (6R,12-6-(1,3-Benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione; (6R,12-6-(Benzo[d][1,3]dioxol-5-yl)-2,3,12,12a-tetrahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4(6H,7H)-dione (Tadalafil Impurity); Tetrahydropalmatine Solution, 100ppm; (6R,12-6-(Benzo[d][1,3]dioxol-5-yl)-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione; N-DesMethyl Tadalafil; CS-0823; Nortadalafil Solution in Methanol, 100μg/mL; (6R-trans)-6-(1,3-Benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione; N-Demethyl Tildenafil; (6R-trans)-6-(1; 12a-hexahydropyrazino[1'; Tildenafil Impurity 7; 4-b]indole-1

物化性质

• 密度: 1.6±0.1 g/cm3
• 沸点: 718.6±60.0 °C at 760 mmHg
• 分子式: C₂₁H₁₇N₃O₄
• 分子量: 375.377
• 闪点: 388.4±32.9 °C
• 精确质量: 375.121918
• PSA: 87.15000
• LogP: 0.38
• 蒸汽压: 0.0±2.3 mmHg at 25°C
• 折射率: 1.772
• 储存条件: 2-8C

生物活性

• 描述: Nortadalafil是demethyl Tadalafil,为PDE5抑制剂。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> 磷酸二酯酶(PDE)
  研究领域 >> 心血管疾病
• 参考文献:

  [1]. Beghyn, et al. PDE5 inhibitors: An original access to novel potent arylated analogues of tadalafil. Bioorganic & Medicinal Chemistry Letters (2007), 17(3), 789-792.

  [2]. Daugan, et al. The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogue. Journal of Medicinal Chemistry (2003), 46(21), 4533-4542.

  [3]. Porst H, et al. Chronic PDE-5 inhibition in patients with erectile dysfunction - a treatment approach using tadalafil once-daily. Expert Opin Pharmacother. 2012 Jul;13(10):1481-94.

  [4]. Frey MK, Lang I. Tadalafil for the treatment of pulmonary arterial hypertension. Expert Opin Pharmacother. 2012 Apr;13(5):747-55.

合成路线

171489-59-1 ~70% 171596-36-4

文献：Beghyn, Terence; Hounsou, Candide; Deprez, Benoit P. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 3 p. 789 - 792

171596-41-1 ~% 171596-36-4

文献：Bioorganic and Medicinal Chemistry Letters, , vol. 17, # 3 p. 789 - 792

4299-70-1 ~% 171596-36-4

文献：Journal of Medicinal Chemistry, , vol. 46, # 21 p. 4533 - 4542

120-57-0 ~% 171596-36-4

文献：Journal of Medicinal Chemistry, , vol. 46, # 21 p. 4533 - 4542

14907-27-8 ~% 171596-36-4

文献：Bioorganic and Medicinal Chemistry Letters, , vol. 17, # 3 p. 789 - 792