(1-Carbamoyl-propyl)-carbamic acid 9H-fluoren-9-ylmethyl ester | 339077-44-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 英文名称: (1-Carbamoyl-propyl)-carbamic acid 9H-fluoren-9-ylmethyl ester
• 英文别名: (9H-Fluoren-9-yl)methyl (1-amino-1-oxobutan-2-yl)carbamate；9H-fluoren-9-ylmethyl N-(1-amino-1-oxobutan-2-yl)carbamate
• CAS: 339077-44-0
• 化学式: C₁₉H₂₀N₂O₃
• 分子量: 324.379
• InChiKey: WAIZVPGKZDAUHU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  24
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  81.4
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  Fmoc-L-苯丙氨酸 、 Fmoc-甘氨酸 、 Fmoc-L-亮氨酸 、 对硝基肉桂酸 、 alkaline earth salt of/the/ methylsulfuric acid 、 (1-Carbamoyl-propyl)-carbamic acid 9H-fluoren-9-ylmethyl ester 在 1-羟基苯并三唑 、 O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate 、 N,N-二异丙基乙胺 、 哌啶 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成
  参考文献：
  名称：

  一种新型拟肽杀虫剂：基于Dippu-AstR的Allatostatin类似物的合理设计和生物活性

  摘要：

  昆虫神经肽在调节昆虫的生长、发育、繁殖、神经传导、代谢和行为方面发挥着重要作用；因此，神经肽的G蛋白偶联受体被认为是设计绿色杀虫剂的重要靶点。蟑螂型尿抑素（AST）（FGLamides allatostatins）是双翅目昆虫中重要的神经肽，可抑制幼体中保幼激素（JH）的合成，影响昆虫的生长、发育和繁殖。因此，寻找针对尿抑素受体（AstR）的新型杀虫剂具有重要意义。此前，我们确定了 AST 类似物H17作为害虫防治的有希望的候选者。在此，我们首先对D. punctata ( Dippu- AstR) 中 AstR 的 3D 结构进行建模，并预测H17与Dippu -AstR 的结合模式，以研究有利于其生物活性的关键相互作用和残基。基于这种结合模式，我们设计并合成了一系列H17衍生物，并评估了它们对点状螨的杀虫活性。其中，化合物Q6通过抑制JH生物合成，对点状昆虫表现出比H17更高的杀虫活性

  DOI：

  10.1021/acs.jafc.3c09231
• 作为产物：
  描述：

  氯甲酸-9-芴基甲酯 、 alkaline earth salt of/the/ methylsulfuric acid 以93%的产率得到(1-Carbamoyl-propyl)-carbamic acid 9H-fluoren-9-ylmethyl ester
  参考文献：
  名称：

  Solid-phase synthesis of amino amides and peptide amides with unnatural side chains

  摘要：

  Unnatural amino amides and peptide amides can be synthesized, using solid-phase chemistry, from glycine attached directly (or through an intervening peptide sequence) to a Rink resin. The glycine is converted to an activated benzophenone imine derivative, followed by C-alkylation and hydrolysis. This sequence provides a mild, high yielding route to Rink resin-bound racemic, unnatural, amino amides and di- and tripeptide amides. Cleavage with trifluoroacetic acid provides the final amide products in good yield and purity. (C) 2001 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0040-4039(01)00090-9

文献信息

• Proteasome inhibitors and methods of using the same
  申请人：Bernadini Raffaella

  公开号：US20050107307A1

  公开（公告）日：2005-05-19

  The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.

  本发明提供了硼酸化合物、硼酸酯及其组合物，可以通过抑制蛋白酶体活性等方式调节细胞凋亡。这些化合物和组合物可以用于诱导细胞凋亡并治疗癌症等疾病，以及与蛋白酶体活性直接或间接相关的其他疾病。
• PROTEASOME INHIBITORS AND METHODS OF USING THE SAME
  申请人：Bernardini Raffaella

  公开号：US20090291918A1

  公开（公告）日：2009-11-26

  The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.

  本发明提供了硼酸化合物、硼酸酯及其组合物，可以调节细胞凋亡，例如通过抑制蛋白酶体活性。这些化合物和组合物可以用于诱导细胞凋亡和治疗癌症及其他与蛋白酶体活性直接或间接相关的疾病。
• Proteasome Inhibitors and Methods of Using the Same
  申请人：Bernardini Raffaella

  公开号：US20120041196A1

  公开（公告）日：2012-02-16

  The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.

  本发明提供了硼酸化合物、硼酸酯及其组合物，可以调节凋亡，例如通过抑制蛋白酶体活性。这些化合物和组合物可以用于诱导凋亡和治疗癌症以及其他与蛋白酶体活性直接或间接相关的疾病的方法。
• Proteasome Inhibitors And Methods Of Using The Same
  申请人：Cephalon, Inc.

  公开号：US20140088042A1

  公开（公告）日：2014-03-27

  The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.

  本发明提供了硼酸化合物、硼酸酯及其组合物，可以调节凋亡，例如通过抑制蛋白酶体活性。这些化合物和组合物可以用于诱导凋亡和治疗癌症和其他与蛋白酶体活性直接或间接相关的疾病的方法。
• SOLID PHASE PEPTIDE SYNTHESIS VIA SIDE CHAIN ATTACHMENT
  申请人：Chemical & Biopharmaceutical Laboratories of Patras S.A.

  公开号：US20140235789A1

  公开（公告）日：2014-08-21

  The present application discloses peptides and peptaibols of high purity may be obtained by solid phase peptide synthesis using as the starting resin hydroxy amino acids, hydroxy amino acid amides, hydroxy amino alcohols or small peptides containing hydroxy amino acids attached to polymers through their side chain.