D-2'-naphthylalanine | 93222-39-0

• 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: D-2'-naphthylalanine
• 英文别名: (R)-(+)-α-N-(2-naphthyl)alanine；2-naphthyl-D-alanine；(R)-2-(naphthalen-2-ylamino)-propionic acid；(D)-(2-naphthyl)alanine；D-2-naphthylalanine；(R)-N-(2-Naphthyl)alanin；(2R)-2-(naphthalen-2-ylamino)propanoic acid
• CAS: 93222-39-0
• 化学式: C₁₃H₁₃NO₂
• 分子量: 215.252
• InChiKey: RWLSBXBFZHDHHX-SECBINFHSA-N

物化性质

• 沸点：
  456.2±28.0 °C(Predicted)
• 密度：
  1.258±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  49.3
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  D-丙氨酸 、 2-萘酚 在 sodium hydrogensulfite 、 sodium sulfite 作用下， 反应 168.0h， 以25%的产率得到D-2'-naphthylalanine
  参考文献：
  名称：

  Preparation of N-(2-naphthyl)-2-amino acids and esters of high enantiomeric purity

  摘要：

  DOI：

  10.1021/jo00351a024

文献信息

• [EN] PEPTIDOMIMETICS FOR IMAGING THE GHRELIN RECEPTOR<br/>[FR] PEPTIDOMIMÉTIQUES POUR IMAGER LE RÉCEPTEUR DE LA GHRÉLINE
  申请人：LONDON HEALTH SCI CT RES INC

  公开号：WO2016191865A1

  公开（公告）日：2016-12-08

  ABSTRACT The present invention concerns compositions comprising and methods of identification and use of imaging agents. The imaging agents comprise a growth hormone secretagogues having a conjugated fluoride. The imaging agents of the present invention may be used for detection, diagnosis and/or staging of prostate or other forms of cancer, and may also be used for cardiac disease.

  摘要 本发明涉及包含成分的组合物，以及用于识别和使用成像剂的方法。这些成像剂包括具有共轭氟化物的生长激素分泌素。本发明的成像剂可用于前列腺或其他形式的癌症的检测、诊断和/或分期，也可用于心脏疾病。
• [EN] DIPHENYLAZETIDINONE DERIVATES POSSESSING CHOLESTEROL ABSORPTION INHIBITORY ACTIVITY<br/>[FR] DERIVES DIPHENYLAZETIDINONE A ACTIVITE INHIBITRICE DE L'ABSORPTION DU CHOLESTEROL
  申请人：ASTRAZENECA AB

  公开号：WO2005061452A1

  公开（公告）日：2005-07-07

  Compounds of formula (I) (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described.

  化合物的结构式（其中变量基团如定义所示）及其药学上可接受的盐、溶剂合物、该类盐的溶剂合物和它们的前药，以及它们作为治疗高脂血症的胆固醇吸收抑制剂的用途被描述。还描述了它们的制备方法和含有它们的药物组合物。
• CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS
  申请人：Obrecht Daniel

  公开号：US20120202821A1

  公开（公告）日：2012-08-09

  Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT 2B (5-HT 2B receptor), and on the prostaglandin F2•receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.

  构象受限、空间定义的12-30环大环环系统(I型)由三个不同的构建模块组成：芳香模板a、构象调节剂b和间隔基团c，如详细描述和索赔中所述。类型(I)的大环可通过并行合成或组合化学方法轻松制备。它们被设计用于与特定生物靶点相互作用。特别是，它们在胃动素受体(MR受体)、5-HT2B亚型的5-羟色胺受体(5-HT2B受体)和前列腺素F2受体(FP受体)上显示出激动或拮抗活性。因此，它们潜在地可用于治疗胃肠道低动力障碍，如糖尿病性胃轻瘫和便秘型肠易激综合征；中枢神经系统相关疾病，如偏头痛、精神分裂症、精神病或抑郁症；眼压增高，如青光眼和早产。
• METHOD FOR SYNTHESIZING OPTICALLY ACTIVE a-AMINO ACID USING CHIRAL METAL COMPLEX COMPRISING AXIALLY CHIRAL N-(2-ACYLARYL)-2-[5,7-DIHYDRO-6H-DIBENZO[c,e]AZEPIN-6-YL] ACETAMIDE COMPOUND AND AMINO ACID
  申请人：HAMARI CHEMICALS, LTD.

  公开号：US20160102045A1

  公开（公告）日：2016-04-14

  Objects of the present invention are to provide an industrially applicable method for producing an optically active α-amino acid in high yield and in a highly enantioselective manner, to provide a simple production method of an optically active α,α-disubstituted α-amino acid, and to provide an intermediate useful for the above production methods of an optically active α-amino acid and an optically active α,α-disubstituted α-amino acid. The present invention provides a production method of an optically active α-amino acid or a salt thereof, the production method comprising introducing a substituent into the α carbon in the α-amino acid moiety of a metal complex represented by the following Formula (1): by an alkylation reaction, an aldol reaction, the Michael reaction, or the Mannich reaction, and releasing an optically pure α-amino acid enantiomer or a salt thereof by acid decomposition of the metal complex.

  本发明的目的是提供一种在高产率和高对映选择性的方式下生产光学活性α-氨基酸的工业上适用的方法，提供一种简单的生产方法，用于光学活性α，α-二取代的α-氨基酸，并提供一种用于上述光学活性α-氨基酸和光学活性α，α-二取代的α-氨基酸生产方法的中间体。本发明提供了一种光学活性α-氨基酸或其盐的生产方法，该生产方法包括通过烷基化反应、醛醇反应、迈克尔反应或曼尼希反应将取代基引入以下式（1）所表示的金属配合物的α-氨基酸基团的α碳中，并通过酸分解金属配合物释放光学纯α-氨基酸对映体或其盐。
• COMPOSITIONS AND METHODS FOR IMAGING CANCER
  申请人：BRITISH COLUMBIA CANCER AGENCY BRANCH

  公开号：US20160333068A1

  公开（公告）日：2016-11-17

  Somatostatin derivative compounds of general formula (I) that may be readily labelled with the isotope fluorine-18 and that have affinity and selectivity for cellular somatostatin receptors are provided. The labelled compounds are useful clinically as radioactive tracers in various in vivo imaging applications (for example, using positron emission tomography (PET) and related techniques) to detect somatostatin-expressing cells and tissues, including tumours, or as therapeutic agents.

  提供了通式（I）的生长抑素衍生物化合物，这些化合物可以很容易地用同位素氟-18标记，并具有对细胞生长抑素受体的亲和力和选择性。这些标记的化合物在临床上可用作放射性示踪剂，用于各种体内成像应用（例如，使用正电子发射断层扫描（PET）和相关技术）来检测表达生长抑素的细胞和组织，包括肿瘤，或作为治疗剂。