N-benzyloxycarbonyldehydrophenylalanine | 84759-65-9

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 肉桂酸及其衍生物
• 英文名称: N-benzyloxycarbonyldehydrophenylalanine
• 英文别名: alpha-Benzyloxycarbonylamino-beta-phenylacrylic acid；3-phenyl-2-(phenylmethoxycarbonylamino)prop-2-enoic acid
• CAS: 84759-65-9
• 化学式: C₁₇H₁₅NO₄
• 分子量: 297.31
• InChiKey: JSQYUMRAVHPDOK-UHFFFAOYSA-N

物化性质

• 熔点：
  160 °C(Solv: ethyl acetate (141-78-6))
• 沸点：
  481.7±45.0 °C(Predicted)
• 密度：
  1.287±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  22
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  75.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  甲醇 、 N-benzyloxycarbonyldehydrophenylalanine 在 4-二甲氨基吡啶 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 以 二氯甲烷 为溶剂， 反应 15.0h， 以7 mg的产率得到α-Amino-zimtsaeure-methylester
  参考文献：
  名称：

  Dorsamin-A’s, Glycerolipids Carrying a Dehydrophenylalanine Ester Moiety from the Seed-Eating Larvae of the Bruchid Beetle Bruchidius dorsalis

  摘要：

  Using a TLC autographic assay for radical-scavenging activity with the ABTS radical, the presence of lipophilic antioxidants in the larvae of the wild bruchid seed beetle Bruchidius dorsalis was detected. Assay-guided fractionation of the CHCl3-soluble fraction of the larvae resulted in the isolation of new glycerolipids, designated dorsamin-A763, -A737, -A765, -A739, and -A767, comprising 1,2-diacyl-sn-glycero-3-dehydrophenylalanine ester structural units. The ABTS radical scavenging activity of the dorsamin-A's was comparable with or stronger than that of Trolox.

  DOI：

  10.1021/np300713c
• 作为产物：
  描述：

  氨基甲酸苄酯 、 苯丙酮酸 在 对甲苯磺酸 作用下， 以 苯 为溶剂， 反应 4.0h， 以1.8 g的产率得到N-benzyloxycarbonyldehydrophenylalanine
  参考文献：
  名称：

  Dorsamin-A’s, Glycerolipids Carrying a Dehydrophenylalanine Ester Moiety from the Seed-Eating Larvae of the Bruchid Beetle Bruchidius dorsalis

  摘要：

  Using a TLC autographic assay for radical-scavenging activity with the ABTS radical, the presence of lipophilic antioxidants in the larvae of the wild bruchid seed beetle Bruchidius dorsalis was detected. Assay-guided fractionation of the CHCl3-soluble fraction of the larvae resulted in the isolation of new glycerolipids, designated dorsamin-A763, -A737, -A765, -A739, and -A767, comprising 1,2-diacyl-sn-glycero-3-dehydrophenylalanine ester structural units. The ABTS radical scavenging activity of the dorsamin-A's was comparable with or stronger than that of Trolox.

  DOI：

  10.1021/np300713c

文献信息

• [EN] NOVEL LACTAMS AND USES THEREOF<br/>[FR] NOUVELLES LACTAMES ET UTILISATIONS DE CES DERNIERES
  申请人：ASTRAZENECA AB

  公开号：WO2004031154A1

  公开（公告）日：2004-04-15

  Compounds having the formula (I) pharmaceutical compositions containing them and their methods of use for the treatment of neurological disorders related to amyloid ß protein production and neurological disorders such as Alzheimer's disease.. These compounds inhibit γ secretase and thereby inhibit the production of amyloid ß protein, thereby acting to prevent the formation of neurological deposits of amyloid protein.

  具有化学式（I）的化合物，含有它们的药物组合物以及它们用于治疗与淀粉样蛋白ß产生相关的神经系统疾病和阿尔茨海默病等神经系统疾病的方法。这些化合物抑制γ-分泌酶，从而抑制淀粉样蛋白ß的产生，从而防止神经系统中淀粉样蛋白的沉积形成。
• Aza hydroxylated ethyl amine compounds utility
  申请人：——

  公开号：US20030229138A1

  公开（公告）日：2003-12-11

  Disclosed are compounds of formula: 1 and pharmaceutically acceptable salts and esters thereof, useful in treating and/or preventing Alzheimer's disease and other similar diseases, wherein R N , R C , R 1 , R 2 and R 20 are defined herein,. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.

  揭示了以下结构的化合物及其药用盐和酯，可用于治疗和/或预防阿尔茨海默病和其他类似疾病，其中RN、RC、R1、R2和R20在此处定义。这些化合物包括β-分泌酶酶抑制剂，可用于治疗阿尔茨海默病和其他在哺乳动物中由Aβ肽沉积所特征的疾病。本发明的化合物可用于制备药物组合物和治疗方法，以减少Aβ肽的形成。
• Novel derivatives of 4,4' dithiobis-(3-aminobutane-1-1-sulfonates) and compositions comprising the same
  申请人：Roques Pierre Bernard

  公开号：US20060205695A1

  公开（公告）日：2006-09-14

  The invention relates to derivatives of 4,4′-dithiobis-(3-aminobutane-1-sulfonates) of formula (1), of use for the treatment and prevention of primary and secondary arterial hypertension.

  本发明涉及公式（1）的4,4'-二硫基双(3-氨基丁烷-1-磺酸酯)的衍生物，用于治疗和预防原发性和继发性动脉高血压。
• Novel lactams and uses thereof
  申请人：Becker Christopher

  公开号：US20060089346A1

  公开（公告）日：2006-04-27

  Compounds having the formula (1) pharmaceutical compositions containing them and their methods of use for the treatment of neurological disorders related to amyloid B protein production and neurological disorders such as Alzheimer's disease. These compounds inhibit γ secretase and thereby inhibit the production of amyloid β protein, thereby acting to prevent the formation of neurological deposits of amyloid protein.

  具有公式（1）的化合物，含有它们的制药组合物，以及它们的使用方法，用于治疗与淀粉样B蛋白产生相关的神经系统疾病和神经系统疾病，例如阿尔茨海默病。这些化合物抑制γ-分泌酶，从而抑制淀粉样β蛋白的产生，从而防止淀粉样蛋白的神经沉积形成。
• Methods of treating alzheimer's disease
  申请人：Schostarez Heinrich

  公开号：US20050130941A1

  公开（公告）日：2005-06-16

  Disclosed are methods for treating Alzheimer's disease, and other diseases, and/or inhibiting beta-secretase enzyme, and/or inhibiting deposition of A beta peptide in a mammal, by use of hydrazine compounds of formula (I) wherein the variables R 1 -R 9 are defined herein.

  本发明涉及使用式(I)中变量R1-R9所定义的肼化合物治疗阿尔茨海默病和其他疾病，抑制β-分泌酶酶活性，抑制A beta肽在哺乳动物体内的沉积。