Z(OMe)-Pro-OH | 38495-86-2

• 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: Z(OMe)-Pro-OH
• 英文别名: (2S)-1-[(4-methoxyphenyl)methoxycarbonyl]pyrrolidine-2-carboxylic acid
• CAS: 38495-86-2
• 化学式: C₁₄H₁₇NO₅
• 分子量: 279.293
• InChiKey: CVSHGODQIJTHKI-LBPRGKRZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  20
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  76.1
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  Z(OMe)-Pro-OH 在 苯甲醚 、 三氟乙酸 、 氯甲酸异丁酯 作用下， 反应 6.0h， 生成 H-Pro-Thr-OMe
  参考文献：
  名称：

  肽的研究。CXXXV。制备用于合成人降钙素基因相关肽（hCGRP）的七个肽片段。

  摘要：

  七个肽片段通过已知的酰胺形成反应合成，作为溶液相合成与人类降钙素基因相关肽（hCGRP）完整氨基酸序列相对应的七十氨基肽酰胺的构建块。采用了S-1-亚当烷基半胱氨酸 [O. Nishimura, C. Kitada, 和 M. Fujino, Chem. Pharm. Bull., 26, 1576 (1978)]，同时使用了具有保护基团的氨基酸衍生物，这些保护基团可通过1 M三氟甲磺酸-硫醇醚在三氟乙酸中去除。

  DOI：

  10.1248/cpb.34.603
• 作为产物：
  描述：

  2-(4-甲氧基苄氧基羰基氧基亚氨基)-2-苯乙腈 、 L-脯氨酸 以92%的产率得到
  参考文献：
  名称：

  CHEN, SHUI-TEIN;WENG, CHIH-SHYONG;WANG, KUNG-TSUNG, J. CHIN. CHEM. SOC., 34,(1987) N 2, 117-123

  摘要：

  DOI：

文献信息

• Studies on peptides. CLXIV. Solution-phase synthesis of a 36-residue peptide amide corresponding to the entire amino acid sequence of chicken antral peptide.
  作者：LILI Guo、EIGORO MURAYAMA、SUSUMU FUNAKOSHI、NOBUTAKA FUJII、MITSURU AONO、MASAYUKI MATSUDA、MOTOYUKI MORIGA、HARUAKI YAJIMA

  DOI：10.1248/cpb.36.4364

  日期：——

  A 36-residue peptide amide corresponding to the entire amino acid sequence of chicken antral peptide was synthesized by assembling seven peptide fragments via the azide, followed by thioanisole-mediated deprotection with trimethylsilyl bromide and trimethylsilyl trifluoromethanesulfonate in trifluoroacetic acid.The synthetic peptide stimulated gastric secretion, but not pancreatic secretion.

  通过叠氮化物组装七个肽片段，然后在三氟乙酸中用三甲基溴硅烷和三氟甲磺酸三甲基硅烷酯介导的硫代茴香醚介导的去保护，合成了对应于鸡胃窦肽的整个氨基酸序列的36个残基的肽酰胺。合成的肽刺激胃液分泌，但不是胰腺分泌。
• Studies on peptides. CLIX. Preparation of a protected 33-residue peptide for the synthesis of human cholecystokinin (hCCK-33).
  作者：NOBUTAKA FUJII、SHIROH FUTAKI、SUSUMU FUNAKOSHI、KENICHI AKAJI、HIROSHI MORIMOTO、OSAMU IKEMURA、HARUAKI YAJIMA

  DOI：10.1248/cpb.36.3271

  日期：——

  A protected 33-residue peptide corresponding to the entire amino acid sequence of human cholecystokinin (hCCK-33) was synthesized by successive azide condensations of 7 peptide fragments of established purity. β-Cycloheptyl aspartate [Asp(OChp)] was employed to suppress base-catalyzed succinimide formation.

  通过连续叠氮化物缩合 7 个已确定纯度的肽片段，合成了对应于人胆囊收缩素 (hCCK-33) 完整氨基酸序列的受保护的 33 个残基肽。 β-环庚基天冬氨酸 [Asp(OChp)] 用于抑制碱催化的琥珀酰亚胺形成。
• New benzopyran compounds with pharmacological activity
  申请人：J. URIACH & CIA. S.A.

  公开号：EP0488301A1

  公开（公告）日：1992-06-03

  The present invention relates to new benzopyranes having the formula I: wherein: R¹ and R² represent, among others, hydrogen, halogen, cyano, C₁₋₄ alkyl, C₁₋₄ alkoxy; R³ is hydrogen or C₁₋₄ alkyl, and R⁴ is C₁₋₄ alkyl, or R³ and R⁴ together form a C₂₋₅ polymethylene chain; R⁵ represents hydroxyl or acetoxy and R⁶ is hydrogen, or R⁵ together with R⁶ form a carbonyl group and R⁷ is hydrogen, or R⁵ and R⁶ together form a bond; R⁷ is hydrogen or C₁₋₆ alkyl; R⁸ is a totally saturated C₅-C₆ cyclic or heterocyclic group selected from cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, piperazinyl, imidazolinyl, pyrazolidinyl, isothiazolidinyl, isoxazolidinyl, thiazolidinyl, oxazolidinyl or morpholinyl, which may be optionally substituted by one or two R⁹ groups; R⁹ is hydroxyl, oxo, C₁₋₆ alkyl, C₁₋₆ alkylcarbonyl, C₁₋₆ alkoxycarbonyl, C₁₋₆ alkoxycarbonylmethyl C₁₋₆ alkylaminocarbonyl, R¹⁰-oxycarbonyl or R¹⁰-(C₁₋₄)alkoxycarbonyl, wherein R¹⁰ is an optionally substituted aryl or heteroaryl group. The invention also relates to a procedure for their preparation and to pharmaceutical compositions containing them. These compounds are antihypertensive and bronchodilator agents.

  本发明涉及具有以下公式I的新苯并吡喃类化合物：其中：R¹和R²代表氢、卤素、氰基、C₁₋₄烷基、C₁₋₄烷氧基等；R³为氢或C₁₋₄烷基，R⁴为C₁₋₄烷基，或R³和R⁴共同形成一个C₂₋₅聚亚甲基链；R⁵代表羟基或乙酰氧基，R⁶为氢，或R⁵和R⁶共同形成一个羰基基团，R⁷为氢，或R⁵和R⁶共同形成一个键；R⁷为氢或C₁₋₆烷基；R⁸为完全饱和的C₅-C₆环状或杂环状基团，选自环戊基、环己基、吡咯烷基、哌啶基、哌嗪基、咪唑啉基、吡唑啉基、异噻唑啉基、异噁唑啉基、噻唑啉基、噁唑啉基或吗啡啉基，可以选择地由一或两个R⁹基团取代；R⁹为羟基、氧代、C₁₋₆烷基、C₁₋₆烷基羰基、C₁₋₆烷氧基羰基甲基、C₁₋₆烷基氨基羰基、R¹⁰-氧代羰基或R¹⁰-(C₁₋₄)烷氧基羰基，其中R¹⁰为可选择地取代的芳基或杂芳基。本发明还涉及它们的制备方法和含有它们的药物组合物。这些化合物是抗高血压和支气管扩张剂。
• Novel aminoglycoside compounds and their acid addition salts and process for production thereof
  申请人：KOWA COMPANY, LTD.

  公开号：EP0134563A1

  公开（公告）日：1985-03-20

  An aminoglycoside compound represented by the following formula (1) wherein R, and R2 are different from each other and each represents a hydrogen atom or a methyl group, R3 represents a hydrogen atom, a hydroxyl group or a methoxy group, A represents a residue of a C2-C11 amino acid or a residue of a dipeptide composed of two said amino acids which are identical or different, and n represents 1 or 2; and its acid addition salt: and a process for the production thereof.

  一种氨基糖苷化合物，由下式（1）表示 其中R和R2互不相同，各自代表氢原子或甲基，R3代表氢原子、羟基或甲氧基，A代表C2-C11氨基酸的残基或由两个相同或不同的上述氨基酸组成的二肽的残基，n代表1或2；及其酸加成盐：以及其生产工艺。
• Tuftsin analogs: synthesis, structure-function relationships, and implications for specificity of tuftsin's bioactivity
  作者：Shlomo Dagan、Philip Gottlieb、Esther Tzehoval、Michael Feldman、Mati Fridkin、Koichi Yasumura、Kenji Okamoto、Haruaki Yajima

  DOI：10.1021/jm00160a027

  日期：1986.10

  Thirteen analogues of the natural macrophage activator peptide tuftsin, ten of which are novel, were synthesized with the aim of exploring the relation between their biological potency and their capacity to attach specifically to cellular tuftsin's receptors. The analogues representing modifications and chain extensions at various parts of the parent tuftsin molecule can be classified as N-terminal analogues, C-terminal analogues, "within-chain" derivatives, or dimers of tuftsin and retrotuftsin. The various synthetic routes employed to prepare the analogues are described. A direct correlation was found between the ability of analogues to inhibit [3H-Arg4]tuftsin specific binding to mice peritoneal macrophages and their capacity to enhance phagocytosis or to inhibit tuftsin-mediated phagocytosis by the cells and to potentiate the cell's immune response.