α-methylene-1-naphthalenepropanoic acid | 139263-24-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: α-methylene-1-naphthalenepropanoic acid
• 英文别名: 1-(α-Naphthylmethyl)acrylic acid；2-(Naphthalen-1-ylmethyl)prop-2-enoic acid
• CAS: 139263-24-4
• 化学式: C₁₄H₁₂O₂
• 分子量: 212.248
• InChiKey: JGYKCUYHXDWYAI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  37.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  α-methylene-1-naphthalenepropanoic acid 在 sodium hydroxide 、 氯化亚砜 作用下， 以 四氢呋喃 、 氯仿 、 N,N-二甲基甲酰胺 为溶剂， 反应 2.0h， 生成 Sodium; 2-(2-acetylsulfanylmethyl-3-naphthalen-1-yl-propionylamino)-ethanesulfonate
  参考文献：
  名称：

  一类新的含有C端磺基的脑啡肽酶抑制剂。

  摘要：

  合成了一系列新的磺酸，并测试了它们对脑啡肽酶的抑制活性。其中，最有效的是N-（2-苄基-3-巯基丙酰基）偏苯甲酸10i，IC50值为0.27 nM。几种其他类似物（10a，b，j，n，o，gg，hh）显示出与C端含脑啡肽酶的C末端抑制剂硫柳芬（IC50 = 2.6 nM）相当或更高的抑制活性。因此，发现含有C端磺基而不是C端羧基的化合物显示出对脑啡肽酶的抑制作用显着高水平。还通过苯基苯醌扭曲试验评价了10b，（S）-10b和（R）-10b的镇痛活性。

  DOI：

  10.1021/jm00081a024
• 作为产物：
  描述：

  2-亚甲基-3-(萘-1-基)丙酸乙酯 在 sodium hydroxide 作用下， 以 1,4-二氧六环 为溶剂， 反应 20.0h， 以90%的产率得到α-methylene-1-naphthalenepropanoic acid
  参考文献：
  名称：

  Mercaptoacyl aminoacid inhibitors of atriopeptidase. 1. Structure-activity relationship studies of methionine and S-alkylcysteine derivatives

  摘要：

  A broad series of N-(3-mercaptoacyl) amino acid derivatives was evaluated for their ability to inhibit atriopeptidase (neutral endopeptidase, EC 3.4.24.11) in vitro and in vivo. Structural parameters studied were (i) the substituent on the 2-position of the 3-mercaptopropionyl moiety, (ii) the amino acid component, (iii) the S-terminal derivative, and (iv) the C-terminal derivative. Optimum activity was observed for derivatives of methionine and S-alkylcysteines. N-[3-Mercapto-2(S)-[(2-methylphenyl)methyl]-1-oxopropyl]-L-methionine was identified as a highly effective inhibitor of atriopeptidase meriting evaluation as a potential cardiovascular therapeutic agent.

  DOI：

  10.1021/jm00041a026

文献信息

• Ni-Catalyzed enantioselective reductive arylcyanation/cyclization of <i>N</i>-(2-iodo-aryl) acrylamide
  作者：Guangzhu Wang、Chaoren Shen、Xinyi Ren、Kaiwu Dong

  DOI：10.1039/d1cc04996h

  日期：——

  A Ni/(S,S)-BDPP-catalyzed intramolecular Heck cyclization of N-(2-iodo-aryl) acrylamide with 2-methyl-2-phenylmalononitrile was developed to give oxindoles with good enantioselectivities. We found that utilizing such an electrophilic cyanation reagent could tackle the deleterious effect of the coordinative cyanide ion in the asymmetric alkene arylcyanation.

  开发了 Ni/( S , S )-BDPP 催化的N -(2-碘代芳基) 丙烯酰胺与 2-甲基-2-苯基丙二腈的分子内 Heck 环化反应，得到具有良好对映选择性的羟吲哚。我们发现使用这种亲电子氰化试剂可以解决配位氰化物离子在不对称烯烃芳基氰化中的有害影响。
• Neutral metalloendopeptidase inhibitors in the treatment of hypertension
  申请人：SCHERING CORPORATION

  公开号：EP0254032A2

  公开（公告）日：1988-01-27

  The method of treating hypertension with neutral metalloendopeptidase (NMEP) inhibitors, NMEP inhibitors in combination with atrial peptides, and NMEP inhibitors in combination with angiotensin converting enzyme inhibitors, as well as pharmaceutical compositions therefor, are disclosed.

  本研究公开了使用中性金属内肽酶（NMEP）抑制剂、NMEP 抑制剂与心房肽联合使用、NMEP 抑制剂与血管紧张素转换酶抑制剂联合使用治疗高血压的方法及其药物组合物。
• Silver halide photographic material comprising monodispersed polymer particles and process for the production thereof
  申请人：MINNESOTA MINING AND MANUFACTURING COMPANY

  公开号：EP0610522A1

  公开（公告）日：1994-08-17

  The present invention relates to a silver halide photographic material having at least one light-sensitive layer coated on a support base and at least one outer light-insensitive layer comprising polydispersed alkali soluble polymer particles and monodispersed alkali insoluble polymer particles having an average particle size of from 1 to 10 µm wherein at least 95% by number of said polymer particles have a diameter within ± 15% of the average particle size.

  本发明涉及一种卤化银感光材料，该材料具有至少一个涂布在支撑基底上的感光层和至少一个感光外层，感光外层包括多分散碱可溶聚合物颗粒和单分散碱不溶聚合物颗粒，其平均粒径为 1 至 10 微米，其中至少 95% 的所述聚合物颗粒的直径（按数量计算）在平均粒径的 ± 15% 以内。
• An optoelectronic semiconductor device
  申请人：SHARP KABUSHIKI KAISHA

  公开号：EP0795941A1

  公开（公告）日：1997-09-17

  A laser or light emitting diode device has a p-i-n structure 3, 4, 5 and a distributed Bragg reflector having layers 6a alternating with layers 6b of different refractive indices. The layers 6a and 6b are formed of p-type conducting polymer materials which are electrically conducting and transparent at the emission wavelength of the device.

  激光器或发光二极管装置具有 pi-n 结构 3、4、5 和分布式布拉格反射器，分布式布拉格反射器具有不同折射率的层 6a 和层 6b。层 6a 和 6b 由 p 型导电聚合物材料构成，在设备的发射波长处具有导电性和透明性。
• Synthesis of a copolymer containing hydrophilic functionality
  申请人：Ferrania S.p.A.

  公开号：EP1408052A1

  公开（公告）日：2004-04-14

  The present invention relates to a process for synthesizing a particulate copolymer comprising: providing a reaction mixture comprising a reaction medium, a polymerization stabilizer, a water-insoluble ethylenically unsaturated monomer and an ethylenically unsaturated monomer containing hydrophilic functionality, and polymerizing the water-insoluble ethylenically unsaturated monomer and the ethylenically unsaturated monomer containing hydrophilic functionality, wherein said reaction mixture has a viscosity value of at least 10 cps measured at 40°C. The polymerization reaction is preferably conducted at a temperature lower than 100°C and activated by a polymerization catalyst. The resulting particulate copolymer dispersion comprises copolymer particles showing a weight average diameter size in the range of microns and absence of defects, such as coagulant or agglomerates. The present invention also provides a dispersion of a particulate copolymer obtained by using the process described above and a photographic material comprising a support and at least one layer containing a particulate copolymer obtained by using the process described above. The photographic material presents improved physical and optical performance.

  本发明涉及一种合成微粒共聚物的工艺，包括：提供一种包含反应介质、聚合稳定剂、不溶于水的乙烯基不饱和单体和含有亲水官能团的乙烯基不饱和单体的反应混合物，以及聚合不溶于水的乙烯基不饱和单体和含有亲水官能团的乙烯基不饱和单体，其中所述反应混合物在 40°C 时测量的粘度值至少为 10 cps。聚合反应最好在低于 100°C 的温度下进行，并由聚合催化剂活化。所得到的微粒共聚物分散体包括重量平均直径尺寸在微米范围内的共聚物微粒，且不存在缺陷，如凝结剂或团聚体。本发明还提供了一种通过上述工艺获得的微粒共聚物分散体和一种感光材料，该感光材料包括一个支架和至少一层含有通过上述工艺获得的微粒共聚物的层。该感光材料具有更好的物理和光学性能。