tert-butyl 2-(((benzyloxy)carbonyl)glycyl)hydrazine-1-carboxylate | 23776-82-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: tert-butyl 2-(((benzyloxy)carbonyl)glycyl)hydrazine-1-carboxylate
• 英文别名: tert-butyl N-[[2-(benzyloxycarbonylamino)acetyl]amino]carbamate；Z-Gly-NH-NH-CO-OtBu；Z-Gly-Gly-NH-NH-CO-OtBu；Z-Gly-NHNH-Boc；tert-butyl 2-({[(benzyloxy)carbonyl]amino}acetyl)hydrazinecarboxylate；benzyl N-({N'-[(tert-butoxy)carbonyl]hydrazinecarbonyl}methyl)carbamate；benzyl N-[2-[2-[(2-methylpropan-2-yl)oxycarbonyl]hydrazinyl]-2-oxoethyl]carbamate
• CAS: 23776-82-1
• 化学式: C₁₅H₂₁N₃O₅
• mdl: MFCD00468755
• 分子量: 323.349
• InChiKey: VYFGJFRMOBUSCX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  23
• 可旋转键数：
  7
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  106
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  tert-butyl 2-(((benzyloxy)carbonyl)glycyl)hydrazine-1-carboxylate 在 盐酸 作用下， 以 1,4-二氧六环 为溶剂， 反应 2.0h， 以1.7 g的产率得到CBZ-甘氨酸酰肼
  参考文献：
  名称：

  [EN] AMINOCARBAMOYL COMPOUNDS FOR THE TREATMENT OF VIRAL INFECTIONS
  [FR] COMPOSÉS AMINOCARBAMOYLE DESTINÉS AU TRAITEMENT D'INFECTIONS VIRALES

  摘要：

  本发明涉及公式（II）中的化合物，其中R1-R5，X和L如本文所述，并其药用盐，包括该化合物的组合物和使用该化合物的方法，特别是用于治疗和预防冠状病毒感染。

  公开号：

  WO2022043374A1
• 作为产物：
  描述：

  肼基甲酸叔丁酯 、 N-苄氧羰基甘氨酸 生成 tert-butyl 2-(((benzyloxy)carbonyl)glycyl)hydrazine-1-carboxylate
  参考文献：
  名称：

  缓激肽-Val-Ala-Pro-Ala-Ser-OH的合成及其生物学特性。

  摘要：

  描述了生物活性肽bradykinyl-Val-Ala-Pro-Ala-Ser-OH的合成。所有片段的缩合均采用Rudinger的叠氮化物方法，以最小化在肽片段耦合步骤中发生的消旋化。随之而来的十四肽在化学和生物性质上与天然来源的bradykinyl-Val-Ala-Pro-Ala-Ser-OH完全相同，并具有高度的均一性。

  DOI：

  10.1248/cpb.21.616

文献信息

• [EN] NOVEL PHENYL IMIDAZOLES AND PHENYL TRIAZOLES AS GAMMA-SECRETASE MODULATORS<br/>[FR] NOUVEAUX PHÉNYL IMIDAZOLES ET PHÉNYL TRIAZOLES EN TANT QUE MODULATEURS DE LA GAMMA SÉCRÉTASE
  申请人：PFIZER

  公开号：WO2010100606A1

  公开（公告）日：2010-09-10

  Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

  所述化合物及其药用可接受盐已被披露，其中所述化合物具有规范中定义的Formula (I)的结构。相应的药物组合物、治疗方法、合成方法和中间体也已被披露。
• Amino Acids and Peptides. XXV. Preparation of Fibronectin-Related Peptide Poly(ethylene glycol) Hybrids and Their Inhibitory Effect on Experimental Metastasis.
  作者：Koichi KAWASAKI、Machiko NAMIKAWA、Yuko YAMASHIRO、Yuji IWAI、Takao HAMA、Yasuo TSUTSUMI、Susumu YAMAMOTO、Shinsaku NAKAGAWA、Tadanori MAYUMI

  DOI：10.1248/cpb.43.2133

  日期：——

  Hybrids of fibronectin-related peptides [Arg-Gly-Asp (RGD), Arg-Gly-Asp-Ser (RGDS)] and poly(ethylene glycol) (PEG) were prepared and their inhibitory effects on experimental metastasis in mice were examined. The inhibitory effect of RGD was markedly potentiated by hybrid formation with poly(ethylene glycol) #6000. As to inhibitory effect, RGD was more potent than RGDS and RGD PEG hybrids were superior to RGDS PEG hybrids. Hybrid formation with PEG #6000 was more effective than that with PEG #4000.

  将整合素连接肽[精-甘-天冬 (RGD)，精-甘-天冬-丝 (RGDS)] 与聚乙二醇 (PEG) 的缀合物制备出来，并研究了它们对小鼠实验性转移的抑制作用。与聚乙二醇 #6000 形成的缀合物显著增强了 RGD 的抑制效果。在抑制作用方面，RGD 比 RGDS 更强，而 RGD PEG 缀合物优于 RGDS PEG 缀合物。与 PEG #4000 相比，与 PEG #6000 形成的缀合物效果更佳。
• Novel Phenyl Imidazoles and Phenyl Triazoles As Gamma-Secretase Modulators
  申请人：Allen Martin Patrick

  公开号：US20120053165A1

  公开（公告）日：2012-03-01

  Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

  本发明公开了具有式（I）所定义的结构的化合物及其药学上可接受的盐，同时公开了相应的制药组合物、治疗方法、合成方法和中间体。
• Aza vinyl sulfones: Synthesis and evaluation as antiplasmodial agents
  作者：Paulo M.C. Glória、Jiri Gut、Lídia M. Gonçalves、Philip J. Rosenthal、Rui Moreira、Maria M.M. Santos

  DOI：10.1016/j.bmc.2011.10.018

  日期：2011.12

  A series of novel aza vinyl sulfones were designed, synthesized in good yields and evaluated as antiplasmodial agents. Tested compounds did not show activity against papain or the Plasmodium falciparum cysteine protease falcipain-2. However, a number of the new compounds effectively inhibited the in vitro development of P. falciparum. Compounds containing a squaramide group were the most active, with IC(50) values between 0.95 and 4.5 mu M, suggesting that these are potential lead compounds for the development of new antimalarial agents. (C) 2011 Elsevier Ltd. All rights reserved.
• Oxadiazole-Based Cell Permeable Macrocyclic Transition State Inhibitors of Norovirus 3CL Protease
  作者：Vishnu C. Damalanka、Yunjeong Kim、Kevin R. Alliston、Pathum M. Weerawarna、Anushka C. Galasiti Kankanamalage、Gerald H. Lushington、Nurjahan Mehzabeen、Kevin P. Battaile、Scott Lovell、Kyeong-Ok Chang、William C. Groutas

  DOI：10.1021/acs.jmedchem.5b01464

  日期：2016.3.10

  Human noroviruses are the primary causative agents of acute gastroenteritis and a pressing public health burden worldwide. There are currently no vaccines or small molecule therapeutics available for the treatment or prophylaxis of norovirus infections. Norovirus 3CL protease plays a vital role in viral replication by generating structural and nonstructural proteins via the cleavage of the viral polyprotein. Thus, molecules that inhibit the viral protease may have potential therapeutic value. We describe herein the structure-based design, synthesis, and in vitro and cell-based evaluation of the first class of oxadiazole-based, permeable macrocyclic inhibitors of norovirus 3CL protease.