tert-butyl 2-(((benzyloxy)carbonyl)leucyl)hydrazine-1-carboxylate | 1312773-78-6

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: tert-butyl 2-(((benzyloxy)carbonyl)leucyl)hydrazine-1-carboxylate
• CAS: 1312773-78-6
• 化学式: C₁₉H₂₉N₃O₅
• 分子量: 379.456
• InChiKey: VVALNADLGHDZOR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.88
• 重原子数：
  27.0
• 可旋转键数：
  6.0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  105.76
• 氢给体数：
  3.0
• 氢受体数：
  5.0

反应信息

• 作为反应物：
  描述：

  tert-butyl 2-(((benzyloxy)carbonyl)leucyl)hydrazine-1-carboxylate 在 palladium 10% on activated carbon 、 氢气 作用下， 以 甲醇 为溶剂， 反应 3.0h， 生成 tert-butyl N-[(2-amino-4-methylpentanoyl)amino]carbamate
  参考文献：
  名称：

  Inhibitors of human neutrophil elastase based on a highly functionalized N-amino-4-imidazolidinone scaffold

  摘要：

  A series of compounds based on the N-amino-4-imidazolidinone scaffold was synthesized and screened against human neutrophil elastase (HNE). These studies lead to the identification of a selective, low micromolar reversible competitive inhibitor of HNE. (C) 2010 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2010.06.028
• 作为产物：
  描述：

  肼基甲酸叔丁酯 、 以 四氢呋喃 为溶剂， 反应 7.0h， 生成 tert-butyl 2-(((benzyloxy)carbonyl)leucyl)hydrazine-1-carboxylate
  参考文献：
  名称：

  Inhibitors of human neutrophil elastase based on a highly functionalized N-amino-4-imidazolidinone scaffold

  摘要：

  A series of compounds based on the N-amino-4-imidazolidinone scaffold was synthesized and screened against human neutrophil elastase (HNE). These studies lead to the identification of a selective, low micromolar reversible competitive inhibitor of HNE. (C) 2010 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2010.06.028

文献信息

• Solution and soluble polymer syntheses of 3-aminoimidazoline-2,4-diones
  作者：Juyoung Yoon、Chang-Woo Cho、Hyunsoo Han、Kim D. Janda

  DOI：10.1039/a807067i

  日期：——

  3-Aminoimidazoline-2,4-dione derivatives have been synthesized from a combination of α- and aza-amino acids by both solution phase and soluble polymer supported approaches; this soluble polymer methodology combines clean product isolation with recycling of the original matrix.

  3-氨基咪唑啉-2,4-二酮衍生物已通过溶液相和可溶性聚合物支载方法从α-氨基酸和氮杂氨基酸的组合中合成；这种可溶性聚合物方法将清洁的产品分离与原始矩阵的回收相结合。
• Synthese von Cystinpeptiden mit Sequenzen aus demC-terminalen Bereich der Humaninsulin-A-Kette
  作者：Helmut Zahn、Edgar Th. J. Fölsche

  DOI：10.1002/jlac.19687160124

  日期：1968.10.22

  Z-Leu-Tyr-Gln-Leu-Glu-Asn-Tyr-Cys(Bzl)-Asn (3) und Z-Ile-Cys(Bzl)-Ser-Leu-Tyr-Gln-Leu-Glu-Asn-Tyr-Cys(Bzl)-Asn (13), die den Sequenzen 17-21, 13-21 und 10-21 in der A-Kette des Humaninsulins entsprechen, wurden durch Fragmentkondensation aufgebaut (vgl. Schema S. 166), durch Behandeln mit Natrium in flüssigem Ammoniak deblockiert und anschließend durch Luftoxydation in die Cystinpeptide 14-16 übergeführt

  部分受保护的半胱氨酸肽Z-Glu（OBu t）-Asn-Tyr-Cys（Bzl）-Asn，Z-Leu-Tyr-Gln-Leu-Glu-Asn-Tyr-Cys（Bzl）-Asn（3）和对应于序列17-21、13-21和10-21的Z -Ile-Cys（Bzl）-Ser-Leu-Tyr-Gln-Leu-Glu-Asn-Tyr-Cys（Bzl）-Asn（13）通过片段缩合建立人胰岛素A链中的α-环糊精（参见方案p.166），通过在液氨中的钠处理将其解封闭，然后通过空气氧化将其转化为胱氨酸肽14-16。
• [EN] AMINOCARBAMOYL COMPOUNDS FOR THE TREATMENT OF VIRAL INFECTIONS<br/>[FR] COMPOSÉS AMINOCARBAMOYLE DESTINÉS AU TRAITEMENT D'INFECTIONS VIRALES
  申请人：HOFFMANN LA ROCHE

  公开号：WO2022043374A1

  公开（公告）日：2022-03-03

  The present invention relates to compounds of formula (II) wherein R1-R5, X and L are as described herein, and pharmaceutically acceptable salts thereof, compositions including the compounds and methods of using the compounds, particularly in the treatment and prophylaxis of coronavirus infection.

  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。
• Synthesis of PHI (peptide histidine isoleucine) and related peptides and immunochemical confirmation of amino acid residue in position 24 of PHI with use of the synthetic peptides
  作者：K. Nokihara、C. Yanaihara、K. Iguchi、S. Fukata、H. Akai、M. Tanaka、T. Mochizuki、K. Tatemoto、V. Mutt、N. Yanaihara

  DOI：10.1021/ja00337a046

  日期：1984.12
• 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.