Boc-Lys(2Cl-Z)-OSu | 66438-39-9

• 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: Boc-Lys(2Cl-Z)-OSu
• 英文别名: Boc-Lys(2-Chloro-Z)-Osu；(2,5-dioxopyrrolidin-1-yl) (2S)-6-[(2-chlorophenyl)methoxycarbonylamino]-2-[(2-methylpropan-2-yl)oxycarbonylamino]hexanoate
• CAS: 66438-39-9
• 化学式: C₂₃H₃₀ClN₃O₈
• 分子量: 511.96
• InChiKey: DLFRCISYWZDQHE-KRWDZBQOSA-N

物化性质

• 密度：
  1.33±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  35
• 可旋转键数：
  14
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  140
• 氢给体数：
  2
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  Boc-Lys(2Cl-Z)-OSu 在 硫化氢 、 三乙胺 、 zinc(II) iodide 作用下， 以 1,4-二氧六环 、 二氯甲烷 为溶剂， 反应 17.67h， 生成 2-[4-[[(2S)-6-[(2-chlorophenyl)methoxycarbonylamino]-2-[(2-methylpropan-2-yl)oxycarbonylamino]hexanoyl]sulfanyl-phenylmethyl]phenoxy]acetic acid
  参考文献：
  名称：

  硫酯树脂接头的另一种制备方法，用于固相合成肽C端硫代酸

  摘要：

  提供了用于肽C-末端硫代酸的固相合成的硫代酯树脂接头的另一种制备方法。

  DOI：

  10.1016/s0040-4039(00)00266-5
• 作为产物：
  描述：

  N-羟基丁二酰亚胺 、 N-叔丁氧羰基-N'-(2-氯苄氧羰基)-L-赖氨酸 在 N,N'-二环己基碳二亚胺 作用下， 以 四氢呋喃 为溶剂， 反应 5.0h， 以84%的产率得到Boc-Lys(2Cl-Z)-OSu
  参考文献：
  名称：

  脑源性神经营养因子二肽模拟物的设计与合成

  摘要：

  构建并合成了脑源性神经营养因子（BDNF）环1和4的低分子模拟物，它们代表N-酰基肽的酰胺和二聚酰胺。这些二肽的序列与神经营养蛋白序列的相应环的β-转弯的中心区域共存，并且酰基是先前氨基酸残基的生物等排体。六亚甲基和七亚甲基二胺用作连接BDNF二聚体模拟物中二肽C端的间隔基。这些物质是通过溶液中的经典肽合成方法合成的，实验室代码为GSB-104（HO-Suc-Ser-Lys-NH2），GSB-106（[HO-Suc-Ser-Lys-NH-（CH2）3- ] 2），GSB-207（HO-Suc-Met-Ser-NH2）和GSB-214（[HO-Suc-Met-Ser-NH-（CH2）7 / 2-] 2）。通过在氧化应激条件下使用永生化海马细胞株HT-22的培养，表明两个环的二聚体模拟物在10（-5）-10（-8）M的浓度范围内均表现出神经保护活性。单体环1模拟的GSB-207在相同浓度下是无

  DOI：

  10.1134/s1068162012030053
• 作为试剂：
  描述：

  1,6-己二胺 、 5-O-苄基 1-O-(4-硝基苯基) (2S)-2-[(2-甲基丙烷-2-基)氧基羰基氨基]戊烷二酸酯 在 Boc-Lys(2Cl-Z)-OSu 、 N,N-二甲基-1,3-二氨基丙烷 、 三氟乙酸 作用下， 反应 1.0h， 以96%的产率得到bis-(γ-benzyl-glutamic acid)hexamethylenediamide
  参考文献：
  名称：

  DIPEPTIDE MIMETICS OF NGF AND BDNF NEUROTROPHINS

  摘要：

  公开号：

  EP2397488B1

文献信息

• Artificial ribonucleases 6. Ribonuclease activity of tetrapeptides based on amino acids involved in the catalytic site of RNase T1
  作者：L. S. Koroleva、A. A. Donina、N. V. Tamkovich、N. A. Kovalev、M. A. Zenkova、V. N. Sil’nikov

  DOI：10.1007/s11172-006-0176-4

  日期：2005.11

  Tetrapeptides based on amino acids involved in the catalytic site of RNase T1 were synthesized. These peptides interact with a 96-mer fragment of HIV-1 RNA, which results in phosphodiester bonds splitting. The efficacy of RNA cleavage depends on the mutual arrangement of oppositely charged amino acids (Glu and Arg or Lys) in a peptide. The introduction of an additional cationic fragment (based on bis-quaternary salts of 1,4-diazabicyclooctane) into an RNase mimetic leads to a considerable increase in the efficiency of RNA depolymerization.

  基于RNase T1催化位点氨基酸的四肽已被合成。这些肽与HIV-1 RNA的96-mer片段相互作用，导致磷酸二酯键断裂。RNA切割的效力取决于相反电荷氨基酸（Glu和Arg或Lys）在肽中的相互排列。将附加的阳离子片段（基于1,4-二氮杂双环[4.2.0]辛烷的双季铵盐）引入模拟RNase的结构中，显著提高了RNA解聚的效率。
• Design, RNA cleavage and antiviral activity of new artificial ribonucleases derived from mono-, di- and tripeptides connected by linkers of different hydrophobicity
  作者：Nikolay Tamkovich、Lyudmila Koroleva、Mikhail Kovpak、Elena Goncharova、Vladimir Silnikov、Valentin Vlassov、Marina Zenkova

  DOI：10.1016/j.bmc.2016.02.007

  日期：2016.3

  A novel series of metal-free artificial ribonucleases (aRNases) was designed, synthesized and assessed in terms of ribonuclease activity and ability to inactivate influenza virus WSN/A33/H1N1 in vitro. The compounds were built of two short peptide fragments, which include Lys, Ser, Arg, Glu and imidazole residues in various combinations, connected by linkers of different hydrophobicity (1,12-diaminododecane

  根据核糖核酸酶活性和体外灭活流感病毒WSN / A33 / H1N1的能力，设计，合成和评估了一系列新型的无金属人工核糖核酸酶（aRNase）。这些化合物由两个短肽片段组成，包括不同组合的Lys，Ser，Arg，Glu和咪唑残基，并通过不同疏水性的接头（1,12-二氨基十二烷或4,9-dioxa-1,12-二氨基十二烷）连接）。这些化合物在生理条件下有效裂解不同的RNA底物，其速率比上述人工核糖核酸酶高三到五倍，并显示出类似RNase A的裂解特异性。具有疏水性1,12-二氨基十二烷接头的aRNase的核糖核酸酶活性比具有4,9-dioxa-1,12-二氨基十二烷接头的aRNase高3–40倍。假定的RNA裂解机制是天然核糖核酸酶的典型机制，即通过aRNase中存在的氨基酸的官能团形成酸/碱对形成一般的酸碱催化作用。裂解的pH曲线证实了这一机理。在生理条件下短暂的病毒悬浮培养后，研究中最活
• Polypeptide derivatives and calcium metabolism improving agent
  申请人：Otsuka Pharmaceutical Co., Ltd.

  公开号：US05204326A1

  公开（公告）日：1993-04-20

  Novel polypeptide derivatives, acid-addition salts thereof and complexes thereof, having the activities for inhibiting bone calcium absorption, for lowering the blood level of calcium, as analgesics, for inhibiting secretion of the gastric juice. Pharmaceutical composition can be prepared by formulating, at least one of the novel polypeptide derivatives, acid-addition salts thereof and complexes thereof, together with a proteolytic enzyme inhibitors and/or pharmaceutically acceptable acids. The pharmaceutical composition are quite effective as agents for curing hypercalcemia, for curing Peget's disease, for curing osteoporosis, analgetic agent, anti-ulcerative agent and the like.

  新型多肽衍生物及其酸加成盐和配合物，具有抑制骨钙吸收、降低血钙水平、作为镇痛剂和抑制胃酸分泌的活性。可以通过将至少一种新型多肽衍生物、其酸加成盐和配合物与蛋白酶抑制剂和/或药用酸一起制剂而成制备药物组合物。该药物组合物对治疗高钙血症、治疗佩吉特病、治疗骨质疏松症、镇痛剂、抗溃疡剂等方面具有相当有效的作用。
• Stabilized Analogs of Thymopentin. 1. 4,5-Ketomethylene Pseudopeptides
  作者：Joseph I. DeGraw、Ronald G. Almquist、Charles K. Hiebert、William T. Colwell、Jac Crase、Takeshi Hayano、Amrit K. Judd、Linda Dousman、R. Lane Smith、William R. Waud、Itsuo Uchida

  DOI：10.1021/jm950803a

  日期：1997.7.1

  The pentapeptide, thymopentin (Arg(1)-Lys(2)-Asp(3)-Val(4)-Tyr(5)) is known for its activity as an immunomodulating drug, but with limited half-life in plasma. In this first paper of a series of three studies, the synthesis of analogs stabilized at the peptide bond between the C-terminal amino acids via insertion of a ketomethylene moiety is described. N-Blocked pseudopeptides containing Val(k)Phe, Ala(k)Phe, and Val(k)Val units were prepared and attached to chloromethyl Merrifield resin via the carboxy terminal. Removal of the N-BOC group by trifluoroacetic acid was followed by sequential coupling with N-BOC dipeptides of aspartic acid to yield resin-bound N-BOC pseudotetrapeptides. Removal of N-BOC and coupling with N-BOC-r-N-tosylarginine followed by total cleavage of blocking groups and resin by HF afforded the target pseudopentapeptides. The analogs were found to compete favorably with thymopentin for binding to CEM cells, but binding was reduced by about 20-30% on average. All analogs showed significant enhancement of half-life versus thymopentin in mouse serum, but most showed only modest improvement in human serum. Insertion of proline or norleucine at position 2 in the chain caused a substantial increase in half-life (3-4-fold), while N-methylnorleucine conferred complete stability in the analogs.
• Ösapay, George; Taylor, John W., Journal of the American Chemical Society, 1990, vol. 112, # 16, p. 6046 - 6051
  作者：Ösapay, George、Taylor, John W.

  DOI：——

  日期：——