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：2024-01-02 18:24:28
• 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
• 英文别名: 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,12aR)-; CS-0823; N-Desmethyl Tadalafil; (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; Tadalafil Impurity 21

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