Boc Tyr D.Met Gly OH | 69612-72-2

• 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: Boc Tyr D.Met Gly OH
• 英文别名: N-(tert-Butoxycarbonyl)-L-tyrosyl-D-methionylglycine；2-[[(2R)-2-[[(2S)-3-(4-hydroxyphenyl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]acetic acid
• CAS: 69612-72-2
• 化学式: C₂₁H₃₁N₃O₇S
• 分子量: 469.559
• InChiKey: DIMZBANHWJFXDX-CVEARBPZSA-N

物化性质

• 沸点：
  823.7±65.0 °C(Predicted)
• 密度：
  1.273±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  32
• 可旋转键数：
  13
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  179
• 氢给体数：
  5
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  Boc Tyr D.Met Gly OH 在 盐酸 、 氨 、 1-羟基苯并三唑 、 溶剂黄146 、 三乙胺 、 N,N'-二环己基碳二亚胺 作用下， 以 甲醇 、 N,N-二甲基甲酰胺 为溶剂， 生成 Tyr D.Met Gly (6H)Phe Pro NH2
  参考文献：
  名称：

  Audigier; Mazarguil; Gout, European Journal of Medicinal Chemistry, 1980, vol. 15, # 2, p. 173 - 177

  摘要：

  DOI：
• 作为产物：
  描述：

  Boc tyrosine 在 sodium hydroxide 、 水 、 1-羟基苯并三唑 、 三乙胺 、 N,N'-二环己基碳二亚胺 作用下， 以 甲醇 、 formamide 、 N,N-二甲基甲酰胺 为溶剂， 生成 Boc Tyr D.Met Gly OH
  参考文献：
  名称：

  Audigier; Mazarguil; Gout, European Journal of Medicinal Chemistry, 1980, vol. 15, # 2, p. 173 - 177

  摘要：

  DOI：

文献信息

• Enkephalin analogs and a process for the preparation thereof
  申请人：Richter Gedeon Vegyeszeti Gyar RT

  公开号：US04339440A1

  公开（公告）日：1982-07-13

  The invention relates to new enkephalin analogues of the general formula (I), Tyr-X-Gly-Phe-Y (I) wherein Tyr, Gly and Phe represent L-tyrosyl, glycyl and L-phenylalanyl residue, respectively, X is glycyl residue or a D-.alpha.-aminocarboxylic acid residue with a lower alkyl, lower thioalkyl or phenyl-(lower)-alkyl side chain, and Y is the residue of an L, D or DL-.alpha.-aminophosphonic acid or L, D or DL-.alpha.-aminosulfonic acid, each having a lower alkyl side chain, and salts thereof. These compounds are prepared according to the invention so that an L-, D- or DL-.alpha.-aminophosphonic acid or an L-, D- or DL-.alpha.-aminosulfonic acid, each bearing a lower alkyl side chain, is coupled in the proper order, as defined by formula (I), with the amino acids and/or peptide fragments each having a removable protecting group on the terminal amino group, the protecting group is split off from the terminal amino group, and the free peptide is isolated as such or in the form of its salt. The new compounds according to the invention selectively modify the catecholamine content of the central nucleus of amygdala, thus they may specifically influence the following functions: food intake, emotionality, social behavior, learning and memory processes.

  该发明涉及一般式(I)的新的脑啡肽类似物，其中Tyr、Gly和Phe分别代表L-酪氨酰基、甘氨酰基和L-苯丙氨酰基残基，X是甘氨酰基或具有较低烷基、较低硫代烷基或苯基-(较低)-烷基侧链的D-α-氨基羧酸残基，Y是具有较低烷基侧链的L、D或DL-α-氨基膦酸或L、D或DL-α-氨基磺酸残基，以及它们的盐。根据该发明制备这些化合物，使得L、D或DL-α-氨基膦酸或L、D或DL-α-氨基磺酸，每个带有较低烷基侧链，按照式(I)所定义的正确顺序与氨基酸和/或肽段偶联，每个具有可去保护基的末端氨基团，保护基从末端氨基团上脱落，游离肽被单独分离或以其盐的形式存在。根据该发明的新化合物选择性地修改杏仁核中枢的儿茶酚胺含量，因此它们可能特异地影响以下功能：食物摄入、情绪、社会行为、学习和记忆过程。
• N-Adamantane-substituted tetrapeptide amides
  申请人：G. D. Searle & Co.

  公开号：US04273704A1

  公开（公告）日：1981-06-16

  N-Adamantane-substituted tetrapeptide amides and the pharmacologically acceptable salts thereof are disclosed herein. These compounds are analogs of enkephalin wherein the methionine or leucine of position 5 has been substituted by an adamantyl amide and the glycine of position 2 has been substituted by various amino acid residues. Optionally the tyrosine of position 1 and the phenylalanine of position 4 may be substituted by various amino acid residues. These compounds exhibit agonist activity at opiate receptor sites and are useful as analgesics.

  本文披露了N-戊二醛基取代的四肽酰胺及其药理学上可接受的盐。这些化合物是镇痛肽恩啡啶的类似物，其中第5位的蛋氨酸或亮氨酸被戊二醛基酰胺取代，第2位的甘氨酸被各种氨基酸残基取代。可选地，第1位的酪氨酸和第4位的苯丙氨酸可以被各种氨基酸残基取代。这些化合物在阿片受体位点表现出激动剂活性，并可用作镇痛剂。
• Cyclohexyl and phenyl substituted enkephalins
  申请人：G. D. Searle & Co.

  公开号：US04407746A1

  公开（公告）日：1983-10-04

  The invention discloses cyclohexyl and phenyl substituted enkephalin derivatives of the formula: ##STR1## Where R.sub.1, R.sub.2, R.sub.4, and R.sub.8 is hydrogen or alkyl of R.sub.3 is alkylthioalkyl or alkylsulfinylalkyl, X is: ##STR2## R.sub.5 is cyclohexylmethyl, phenylmethyl, optionally substituted by --NO.sub.2, R.sub.6 is cyclohexyl or phenyl optionally substituted by R.sub.7 and R.sub.7 is hydrogen, an alkyl ester of carboxylic acid or hydroxyalkyl and the pharmaceutically acceptable salts, which are useful as analgesic agents.

  本发明揭示了公式：##STR1##中的环己基和苯基取代的脑啡肽衍生物，其中R.sub.1，R.sub.2，R.sub.4和R.sub.8为氢或烷基，R.sub.3为烷基硫醇基或烷基亚砜基基，X为：##STR2##，R.sub.5为环己基甲基，苯基甲基，可选地取代为--NO.sub.2，R.sub.6为环己基或苯基，可选地取代为R.sub.7，R.sub.7为氢，羧酸酯的烷基或羟基烷基及其药学上可接受的盐，其作为镇痛剂。
• Tetrapeptidehydrazide derivatives
  申请人：Takeda Chemical Industries, Ltd

  公开号：US04277394A1

  公开（公告）日：1981-07-07

  Novel tetrapeptidehydrazide derivatives, inclusive of a pharmacologically acceptable acid addition salt thereof, which has the general formula (I): ##STR1## [wherein R.sub.1 is hydrogen or lower alkyl; R.sub.2 is hydrogen or the side chain of a D-.alpha.-amino acid; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is hydrogen, or a saturated or unsaturated and straight or branched lower aliphatic acyl group which may optionally be substituted by hydroxy, amino, lower alkoxy, halogen, oxo, lower alkylthio or lower alkylthiooxide], are useful as analgesics.

  具有以下一般式（I）的新型四肽酸酐衍生物，包括其药学上可接受的酸盐： ##STR1## [其中R.sub.1是氢或低级烷基；R.sub.2是氢或D-.alpha.-氨基酸的侧链；R.sub.3是氢或低级烷基；R.sub.4是氢，或饱和或不饱和的直链或支链低级脂肪酰基，该基团可以选择性地被羟基，氨基，低级烷氧基，卤素，氧代，低级烷硫基或低级烷硫氧化物取代]，可用作镇痛剂。
• Tetrapeptidesemicarbazide derivatives and their production and use
  申请人：Takeda Chemical Industries, Ltd.

  公开号：US04337247A1

  公开（公告）日：1982-06-29

  Novel tetrapeptidesemicarbazide derivatives, inclusive of a pharmacologically acceptable salt thereof, which has the general formula (I): ##STR1## wherein R.sub.1 is hydrogen or lower alkyl; R.sub.2 is hydrogen or a D-.alpha.-amino acid side chain; R.sub.3 is hydrogen or lower alkyl; X is oxygen or sulfur, are useful as analgesics.

  具有一般式（I）的新型四肽半脲衍生物，包括其药学上可接受的盐，其中R.sub.1为氢或低碳基；R.sub.2为氢或D-.alpha.-氨基酸侧链；R.sub.3为氢或低碳基；X为氧或硫，可用作镇痛剂。