5-methyl-1-trityl-1H-tetrazole

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 英文名称: 5-methyl-1-trityl-1H-tetrazole
• 英文别名: 5-methyl-1-trityl-tetrazole；5-methyl-1-trityltetrazole
• 化学式: C₂₁H₁₈N₄
• 分子量: 326.401
• InChiKey: ORVHDKJGIHRMLB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  43.6
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5-methyl-1-trityl-1H-tetrazole 在 萘 、 lithium 作用下， 以 四氢呋喃 为溶剂， 反应 2.5h， 以93%的产率得到5-甲基四氮唑
  参考文献：
  名称：

  Detritylation of Protected Tetrazoles by Naphthalene-Catalyzed Lithiation

  摘要：

  DOI：

  10.1055/s-0033-1338623
• 作为产物：
  描述：

  5-甲基四氮唑 、 三苯基氯甲烷 在 4-二甲氨基吡啶 、 三乙胺 作用下， 以 二氯甲烷 为溶剂， 以69%的产率得到5-methyl-1-trityl-1H-tetrazole
  参考文献：
  名称：

  Detritylation of Protected Tetrazoles by Naphthalene-Catalyzed Lithiation

  摘要：

  DOI：

  10.1055/s-0033-1338623

文献信息

• BETA-SUBSTITUTED GAMMA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS
  申请人：QUADRIGA BIOSCIENCES, INC.

  公开号：US20150218085A1

  公开（公告）日：2015-08-06

  β-Substituted γ-amino acids, β-substituted γ-amino acid derivatives, and β-substituted γ-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates, capable of passing through the blood-brain barrier, and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres and methods of using the compounds for treating tumors are also disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an improved selectivity toward tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an increased efficacy on a variety of tumor types.

  β-取代的γ-氨基酸，β-取代的γ-氨基酸衍生物，以及β-取代的γ-氨基酸类似物和（生物）同位素及其作为化疗药物的用途被披露。这些β-取代的γ-氨基酸衍生物和β-取代的γ-氨基酸类似物和（生物）同位素是选择性LAT1/4F2hc底物，能够穿过血脑屏障，并在表达LAT1/4F2hc转运蛋白的肿瘤中表现出快速摄取和保留。还披露了合成β-取代的γ-氨基酸衍生物和β-取代的γ-氨基酸类似物和（生物）同位素的方法以及使用这些化合物治疗肿瘤的方法。这些β-取代的γ-氨基酸衍生物和β-取代的γ-氨基酸类似物和（生物）同位素表现出对表达LAT1/4F2hc转运蛋白的肿瘤细胞的改进选择性，并在体内给予受试者时在癌细胞中积累。这些β-取代的γ-氨基酸衍生物和β-取代的γ-氨基酸类似物和（生物）同位素在多种肿瘤类型上表现出增加的疗效。
• ANGIOTENSIN II RECEPTOR BLOCKER DERIVATIVES
  申请人：Almirante Nicoletta

  公开号：US20110052674A1

  公开（公告）日：2011-03-03

  New angiotensin II receptor blocker nitroderivatives of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof: and their use for treating cardiovascular, renal and chronic liver diseases, inflammatory processes and metabolic syndromes.

  新的血管紧张素II受体拮抗剂，通式为(I)和其药学上可接受的盐或立体异构体：以及它们用于治疗心血管，肾脏和慢性肝脏疾病，炎症过程和代谢综合征。
• β-substituted γ-amino acids and analogs as chemotherapeutic agents
  申请人：QUADRIGA BIOSCIENCES, INC.

  公开号：US09394236B2

  公开（公告）日：2016-07-19

  β-Substituted γ-amino acids, β-substituted γ-amino acid derivatives, and β-substituted γ-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates, capable of passing through the blood-brain barrier, and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres and methods of using the compounds for treating tumors are also disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an improved selectivity toward tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an increased efficacy on a variety of tumor types.

  本发明公开了β-取代γ-氨基酸、β-取代γ-氨基酸衍生物以及β-取代γ-氨基酸类似物和(bio)等同物作为化疗药物的用途。β-取代γ-氨基酸衍生物和β-取代γ-氨基酸类似物和(bio)等同物是选择性的LAT1/4F2hc底物，能够通过血脑屏障，并在表达LAT1/4F2hc转运蛋白的肿瘤中表现出快速摄取和保留。本发明还公开了合成β-取代γ-氨基酸衍生物和β-取代γ-氨基酸类似物和(bio)等同物的方法以及使用这些化合物治疗肿瘤的方法。β-取代γ-氨基酸衍生物和β-取代γ-氨基酸类似物和(bio)等同物表现出对表达LAT1/4F2hc转运蛋白的肿瘤细胞的选择性改善，并在体内给予受试者时在癌细胞中积累。β-取代γ-氨基酸衍生物和β-取代γ-氨基酸类似物和(bio)等同物在多种肿瘤类型上表现出更高的疗效。
• US9394236B2
  申请人：——

  公开号：US9394236B2

  公开（公告）日：2016-07-19
• US9682921B2
  申请人：——

  公开号：US9682921B2

  公开（公告）日：2017-06-20