2,3-Dihydroxy-phenyl-ethylamin | 579-59-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2,3-Dihydroxy-phenyl-ethylamin
• 英文别名: 2,3-Dihydroxy-phenaethylamin；2,3-Dihydroxyphenethylamin；3-(2-Aminoethyl)benzene-1,2-diol
• CAS: 579-59-9
• 化学式: C₈H₁₁NO₂
• mdl: MFCD08448779
• 分子量: 153.181
• InChiKey: SYHVBRQKMHIAJQ-UHFFFAOYSA-N

物化性质

• 沸点：
  320.9±27.0 °C(Predicted)
• 密度：
  1.247±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  66.5
• 氢给体数：
  3
• 氢受体数：
  3

安全信息

• 海关编码：
  2922299090

反应信息

• 作为反应物：
  描述：

  3,4,5-三甲氧基苯乙醛 、 2,3-Dihydroxy-phenyl-ethylamin 以75%的产率得到
  参考文献：
  名称：

  YAMADA KOICHIRO; IKEZAKI MUNEYOSHI; UMINO NORIHIDE; OHTSUKA HISAO; ITOH N+, CHEM. AND PHARM. BULL., 1981, 29, NO 3, 744-753

  摘要：

  DOI：
• 作为产物：
  描述：

  2,3-二甲氧基苯甲醛 在 platinum(IV) oxide 盐酸 、 lithium aluminium tetrahydride 、 氯化亚砜 、 氢气 、 三氯化铁 作用下， 以 乙醇 、 水 为溶剂， 生成 2,3-Dihydroxy-phenyl-ethylamin
  参考文献：
  名称：

  Reactions of Isopropyl Methylphosphonofluoridate with Substituted Phenols. II

  摘要：

  DOI：

  10.1021/ja01076a043

文献信息

• Phenylethylamines and condensed rings variants as prodrugs of catecholamines, and their use
  申请人：——

  公开号：US20030087948A1

  公开（公告）日：2003-05-08

  Compounds of the general formula I 1 wherein rings B, C, D and E may be present or not and, when present, are combined with A as A+C, A+E, A+B+C, A+B+D, A+B+E, A+C+E, A+B+C+D or A+B+C+D+E, rings B, C and E being aliphatic whereas ring D may be aliphatic or aromatic/hetero-aromatic, and wherein X is —(CH 2 ) m —, in which m is an integer 1-3, to form a ring E or, when E is absent, a group R 1 bound to the nitrogen atom, wherein R 1 is selected from the group consisting of a hydrogen atom, alkyl or haloalkyl groups of 1 to 3 carbon atoms, cycloalkyl(alkyl) groups of 3 to 5 carbon atoms (i.e. including cyclopropyl, cyclopropylmethyl, cyclobutyl and cyclobutylmethyl) and wherein Y is —(CH 2 ) n —, in which n is an integer 1-3, to form a ring C or when C is absent, a group R 2 bound to the nitrogen atom, wherein R 2 is selected from the group consisting of a hydrogen atom, alkyl or haloalkyl groups of 1 to 7 carbon atoms, cycloalkyl(alkyl) groups of 3 to 7 carbon atoms, alkenyl or alkylnyl groups of 3 to 6 carbon atoms, arylalkyl, heteroarylalkyl having 1 to 3 carbon atoms in the alkyl moiety, whilst the aryl/heteroaryl nucleus may be substituted, provided that when rings B, C, D and E are absent NR 1 R 2 is different from dimethylamino, N-methyl-N-ethylamino, N-methyl-N-propynyl-amino, N-methyl-N-propylamino and N-hydroxipropyl-N-methylamino, and salts thereof with pharmaceutically acceptable acids or bases are disclosed as well as the use of such compounds for the manufacturing of pharmaceutical compositions for the treatment of Parkinson's disease, psychoses, Huntington's disease, impotence, renal failure, heart failure or hypertension, such pharmaceutical compositions and methods of treating Parkinson's disease and schizophrenia.

  通式I的化合物 其中环B、C、D和E可能存在也可能不存在，当存在时，与A结合为A+C、A+E、A+B+C、A+B+D、A+B+E、A+C+E、A+B+C+D或A+B+C+D+E，环B、C和E为脂肪环，而环D可以是脂肪环或芳香/杂环，其中X为—(CH 2 ) m —，其中m为1-3的整数，形成环E或者当E不存在时，与氮原子结合的基团R 1 ，其中R 1 选自氢原子、1至3个碳原子的烷基或卤代烷基基团、3至5个碳原子的环烷基(烷基)基团（即包括环丙基、环丙基甲基、环丁基和环丁基甲基），Y为—(CH 2 ) n —，其中n为1-3的整数，形成环C或者当C不存在时，与氮原子结合的基团R 2 ，其中R 2 选自氢原子、1至7个碳原子的烷基或卤代烷基基团、3至7个碳原子的环烷基(烷基)基团、3至6个碳原子的烯基或烷基基团、芳基烷基、杂环芳基烷基，其中烷基部分含有1至3个碳原子，而芳基/杂环芳基核可能被取代，前提是当环B、C、D和E不存在时，NR 1 R 2 与二甲氨基、N-甲基-N-乙基氨基、N-甲基-N-丙炔基氨基、N-甲基-N-丙基氨基和N-羟基丙基-N-甲基氨基不同，并且还披露了这些化合物与药学上可接受的酸或碱的盐以及用于制造治疗帕金森病、精神病、亨廷顿病、阳痿、肾衰竭、心力衰竭或高血压的药物组合物的用途，以及治疗帕金森病和精神分裂症的药物组合物和方法。
• MODIFIER FOR AROMATIC POLYESTER AND AROMATIC POLYESTER RESIN COMPOSITION COMPRISING THE SAME
  申请人：TABATA Masayoshi

  公开号：US20110224343A1

  公开（公告）日：2011-09-15

  The present invention provides a modifier for aromatic polyesters which enhances the melt fluidity of aromatic polyesters without a significant decrease in the heat resistance of the aromatic polyesters, and an aromatic polyester resin composition including the modifier for aromatic polyesters. The present invention relates to a modifier for aromatic polyesters comprising polyhydric phenol residues and residues of aromatic polycarboxylic acid, acid halide or acid anhydride thereof, and the modifier comprises a material having a structure composed of a first residue selected from the group consisting of divalent residues represented by Formula (I): —Ar—W 1 x —Ar— and by Formula (II): —Ar—, the first residues being bonded to two identical or different second residues selected from the group consisting of monovalent residues represented by Formula (III): and monovalent residues represented by Formula (IV): —O—C(O)—R 7 —.

  本发明提供了一种用于芳香族聚酯的改性剂，可以增强芳香族聚酯的熔融流动性，而不明显降低芳香族聚酯的耐热性，以及包括该改性剂的芳香族聚酯树脂组合物。本发明涉及一种用于芳香族聚酯的改性剂，包括多羟基酚残基和芳香族多羧酸、酸卤或其酸酐残基，该改性剂包括具有以下结构的材料：第一残基，选择自由式(I)所代表的二价残基：—Ar—W1x—Ar—和自由式(II)所代表的：—Ar—，第一残基与选择自由式(III)所代表的单价残基：和自由式(IV)所代表的单价残基：—O—C(O)—R7—的两个相同或不同的第二残基结合。
• Synthesis of phenethylamines from phenylacetonitriles obtained by alkylation of cyanide ion with mannich bases from phenols and other benzylamines
  作者：J.H. Short、D.A. Dunnigan、C.W. Ours

  DOI：10.1016/0040-4020(73)80127-9

  日期：1973.1

  alkylating agents. With such compounds it was necessary to prepare the quaternary salts before alkylation could be achieved. 6-Hydroxydopamine was prepared from 2,4,5-trimethoxybenzaldehyde utilizing the latter approach. 3,5-Dimethoxy-4-hydroxyphenethylamine was cyclized to the corresponding dihydroisoquinoline. The isoquinoline and tetrahydroisoquinoline analogs were also prepared. 4-Hydroxy-3-met

  通过在酚上进行曼尼希反应或通过醛的还原烷基化获得的苄胺已代替苄基氯用于氰化氰离子化，从而获得可还原为苯乙胺的腈。来自伯，仲和叔胺的4-羟基-3-甲氧基苯基乙腈的产率大致相同。没有邻位或对位的苄胺OH基团不充当烷基化剂。对于此类化合物，必须先制备季盐，然后才能实现烷基化。使用后一种方法由2,4,5-三甲氧基苯甲醛制备6-羟基多巴胺。将3，5-二甲氧基-4-羟基苯乙胺环化为相应的二氢异喹啉。还制备了异喹啉和四氢异喹啉类似物。将4-羟基-3-甲氧基苯基乙腈水解为高香草酸，即多巴胺的天然代谢产物。
• BROMODOMAIN LIGANDS CAPABLE OF DIMERIZING IN AN AQUEOUS SOLUTION, AND METHODS OF USING SAME
  申请人：Coferon, Inc.

  公开号：US20140243286A1

  公开（公告）日：2014-08-28

  Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.

  本文介绍了一种单体，当在水介质中与一个、两个、三个或更多其他单体接触时，能够形成生物上有用的多聚体。在其中一方面，这种单体可以在水介质中（例如在体内）与另一个单体结合形成多聚体（例如二聚体）。考虑到的单体可能包括配体基团、连接元素和连接配体基团和连接元素的连接元素。在水介质中，这些考虑到的单体可以通过每个连接元素连接在一起，因此可以同时调节一个或多个生物分子，例如调节蛋白质或不同蛋白质上的两个或更多结合结构域。
• 1,2,4-Triazole-3-thione analogues with an arylakyl group at position 4 as metallo-β-lactamase inhibitors
  作者：Laurent Gavara、Federica Verdirosa、Laurent Sevaille、Alice Legru、Giuseppina Corsica、Lionel Nauton、Paola Sandra Mercuri、Filomena Sannio、Filomena De Luca、Margot Hadjadj、Giulia Cerboni、Yen Vo Hoang、Patricia Licznar-Fajardo、Moreno Galleni、Jean-Denis Docquier、Jean-François Hernandez

  DOI：10.1016/j.bmc.2022.116964

  日期：2022.10

  group of various lengths up to a butyl chain were also synthesized. Some compounds in both sub-series were micromolar to submicromolar inhibitors of tested VIM-type MBLs. A few of them were broad-spectrum inhibitors, as they showed significant inhibitory activity on NDM-1 and, to a lesser extent, IMP-1. Among these, several inhibitors were able to significantly reduce the meropenem MIC on VIM-1- and VIM-4-

  金属-β-内酰胺酶 (MBL) 对公众健康构成越来越严重的威胁，因为它们在全球范围内在相关机会性革兰氏阴性病原体中的流行率增加。MBL 可有效灭活广泛使用且最有价值的 β-内酰胺类抗生素，例如氧亚氨基头孢菌素（头孢曲松、头孢他啶）和最后的碳青霉烯类。迄今为止，还没有 MBL 抑制剂被批准用于治疗应用。我们正在开发以 1,2,4-三唑-3-硫酮支架为原始锌配体特征的抑制剂，并且已经报道了一些有前途的系列。在这里，我们介绍了一系列新化合物的合成和评估，这些化合物的特征是在三唑环的 4 位存在芳基烷基取代基。烷基链主要是乙烯，但也合成了一些不含烷基或具有不同长度的烷基（直至丁基链）的化合物。两个子系列中的一些化合物是测试的 VIM 型 MBL 的微摩尔到亚微摩尔抑制剂。其中一些是广谱抑制剂，因为它们对 NDM-1 和 IMP-1 表现出显着的抑制活性。其中，几种抑制剂能够将美罗培南对产生 VIM-1