3-iodo-α-methyl-DL-tyrosine | 779-96-4

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 苯丙酸
• 英文名称: 3-iodo-α-methyl-DL-tyrosine
• 英文别名: 3-iodo-L-α-methyl-tyrosine；DL-3-Iodo-α-methyltyrosine；3-Iodo-alpha-methyltyrosine；2-amino-3-(4-hydroxy-3-iodophenyl)-2-methylpropanoic acid
• CAS: 779-96-4
• 化学式: C₁₀H₁₂INO₃
• 分子量: 321.115
• InChiKey: KPOIUSXAPUHQNA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.9
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  83.6
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  消旋甲酪氨酸 在 ammonium hydroxide 、 碘 、 potassium iodide 作用下， 生成 3-iodo-α-methyl-DL-tyrosine
  参考文献：
  名称：

  酪氨酸羟化酶抑制剂。取代的芳香族氨基酸的合成和活性。

  摘要：

  DOI：

  10.1021/jm00318a005

文献信息

• [EN] PROTEASOME INHIBITING ß-LACTAM PRODRUGS USEFUL FOR THE TREATMENT OF CANCER AND NEURODEGENERATIVE DISORDERS<br/>[FR] PROMÉDICAMENTS À BASE DE SS-LACTAME INHIBITEURS DU PROTÉASOME UTILES POUR LE TRAITEMENT DU CANCER ET DE TROUBLES NEURODÉGÉNÉRATIFS
  申请人：VITA API

  公开号：WO2018115497A1

  公开（公告）日：2018-06-28

  The present invention relates generally to proteasome inhibiting β-lactam compounds useful for the treatment of cancer and neurodegenerative disorders. The invention also provides pharmaceutical compositions and extended release formulations of said compounds, and medical uses of said compounds and/or pharmaceutical compositions to treat cancer and neurodegenerative disorders.

  本发明通常涉及抑制蛋白酶体的β-内酰胺化合物，用于治疗癌症和神经退行性疾病。该发明还提供了所述化合物的药物组合物和延长释放配方，以及利用所述化合物和/或药物组合物治疗癌症和神经退行性疾病的医疗用途。
• PROTEASOME INHIBITING SS-LACTAM PRODRUGS USEFUL FOR THE TREATMENT OF CANCER AND NEURODEGENERATIVE DISORDERS
  申请人：VITA API

  公开号：EP3339291A1

  公开（公告）日：2018-06-27

  The present invention relates generally to proteasome inhibiting β-lactam compounds useful for the treatment of cancer and neurodegenerative disorders. The invention also provides pharmaceutical compositions and extended release formulations of said compounds, and medical uses of said compounds and/or pharmaceutical compositions to treat cancer and neurodegenerative disorders.

  本发明一般涉及用于治疗癌症和神经退行性疾病的蛋白酶体抑制β-内酰胺化合物。本发明还提供了所述化合物的药物组合物和缓释制剂，以及所述化合物和/或药物组合物治疗癌症和神经退行性疾病的医学用途。
• Proteasome inhibiting β-lactam prodrugs useful for the treatment of cancer and neurodegenerative disorders
  申请人：Vita Api

  公开号：US11053249B2

  公开（公告）日：2021-07-06

  The present invention relates generally to proteasome inhibiting β-lactam compounds useful for the treatment of cancer and neurodegenerative disorders. The invention also provides pharmaceutical compositions and extended release formulations of said compounds, and medical uses of said compounds and/or pharmaceutical compositions to treat cancer and neurodegenerative disorders.

  本发明一般涉及用于治疗癌症和神经退行性疾病的蛋白酶体抑制β-内酰胺化合物。本发明还提供了所述化合物的药物组合物和缓释制剂，以及所述化合物和/或药物组合物治疗癌症和神经退行性疾病的医学用途。
• Electrophilic radioiodination of tyrosine derivatives
  作者：K. Farah、N. Farouk

  DOI：10.1002/(sici)1099-1344(199804)41:4<255::aid-jlcr89>3.3.co;2-f

  日期：1998.4

  A comparative study on the electrophilic radioiodination of L-tyrosine, L-alpha-methyl tyrosine and L-tyrosine methyl ester has been carried out using chloramine-T (CAT) and iodogen as oxidizing agents to generate electrophilic radioiodine. Optimization of the radioiodination conditions has been performed resulting in high labelling yields within short reaction times at room temperature. Radiochromatograms also revealed side product impurities at longer reaction time and higher oxidizing agent concentration. Maximum yields of 93%, 90% and 78% were obtained in case of CAT, while 87%, 88% and 53% were obtained in case of iodogen for L-3-[I-131] iodotyrosine, L-3-[I-131] iodo-a-methyl tyrosine and L-3-[I-131] iodotyrosine methyl ester respectively.
• EP3749290A1
  申请人：——

  公开号：EP3749290A1

  公开（公告）日：2020-12-16