2-乙胺基噻吩 | 203730-54-5

• 物质功能分类: 医药中间体 - 杂环化合物 - 噻吩类化合物
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩类
• 中文名称: 2-乙胺基噻吩
• 英文名称: ethyl-[2]thienyl-amine
• 英文别名: Aethyl-[2]thienyl-amin；Thienylethylamine；thien-2-ylethylamine；2-thienylethylamine；N-Ethylthiophen-2-amine
• CAS: 203730-54-5
• 化学式: C₆H₉NS
• 分子量: 127.21
• InChiKey: BYGZVEKTHREAGM-UHFFFAOYSA-N

物化性质

• 沸点：
  210.5±13.0 °C(Predicted)
• 密度：
  1.107±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  8
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  40.3
• 氢给体数：
  1
• 氢受体数：
  2

安全信息

• 海关编码：
  2934999090

反应信息

• 作为反应物：
  描述：

  2-乙胺基噻吩 、 2,(S)-α-dichlorphenyl-acetic acid (R)-1-(dimethylamino)-2-propyl ester 、 2,(R)-α-dichlorphenyl-acetic acid (R)-1-(dimethylamino)-2-propyl ester 在 三乙胺 作用下， 以 乙腈 为溶剂， 反应 2.0h， 生成 (S)-(2-chlorophenyl)-α-2-[(2-thieno)ethyl]amino-acetic acid (R)-1-(dimethylamino)-2-propyl ester 、 (R)-(2-chlorophenyl)-α-2-[(2-thieno)ethyl]amino-acetic acid (R)-1-(dimethylamino)-2-propyl ester
  参考文献：
  名称：

  Stereoselektives Verfahren zur Herstellung von Clopidogrel

  摘要：

  公开号：

  EP1589019B1
• 作为产物：
  描述：

  噻吩胺 、 乙醛 在 sodium tetrahydroborate 作用下， 以 乙醇 为溶剂， 反应 2.0h， 以4.5 g的产率得到2-乙胺基噻吩
  参考文献：
  名称：

  着色組成物、インクジェット用インク、及び捺染方法

  摘要：

  这段文本描述了一种优异的青色光学密度（OD值）和优异的耐光性的着色组合物，包括含有该着色组合物的喷墨墨水、以及使用该着色组合物或该喷墨墨水的印刷方法。该着色组合物包含一种由公式（1）表示的化合物，喷墨墨水中含有该着色组合物。

  公开号：

  JP2017149805A

文献信息

• [EN] INDAZOLE COMPOUNDS AS KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME<br/>[FR] COMPOSÉS INDAZOLE UTILISÉS COMME INHIBITEURS DE KINASE ET MÉTHODE DE TRAITEMENT DU CANCER AVEC LESDITS COMPOSÉS
  申请人：UNIV HEALTH NETWORK

  公开号：WO2013053051A1

  公开（公告）日：2013-04-18

  The present teaching provide indazole compounds represented by Structural Formulae (I) or (I') or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof as protein kinase inhibitors, such as TTK protein kinase, polo-like kinase 4 (PLK4) and Aurora kinases having anticancer activity against breast cancer cells, colon cancer cells, and ovarian cancer cells.

  本教学提供了由结构式（I）或（I'）表示的吲唑化合物或其药用可接受的盐。还描述了这些药物组合物及其用作蛋白激酶抑制剂的方法，如对乳腺癌细胞、结肠癌细胞和卵巢癌细胞具有抗癌活性的TTK蛋白激酶、极化样激酶4（PLK4）和极化激酶。
• Pharmaceutically active pyrrolidine derivatives
  申请人：——

  公开号：US20030212012A1

  公开（公告）日：2003-11-13

  The present invention is related to pyrrolidine derivatives of formula (I). Said 1 compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including premature labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation, wherein X is selected from the group consisting of CR6R7, NOR6, NNR6R7; A is selected from the group consisting of —(C═O)—, —(C═O)—O—, —C(═NH)—, —(C═O)—NH—, —(C═S)—NH, —SO22—, —SO2NH—, —CH2—,B is either a group —(C═O)—NR8R9 or represents a heterocyclic residue having the formula (a) wherein Q is NR10, O or S; n is an integer selected of 0, 1 or 2; Y, Z and E form together with the 2 carbons to which they are attached a 5-6 membered aryl or heteroaryl ring.

  本发明涉及式(I)的吡咯烷衍生物。所述化合物优选用作药用活性化合物。具体而言，式(I)的吡咯烷衍生物在治疗和/或预防早产、早产和痛经方面是有用的。特别是，本发明涉及显示出氧催产素受体显著调节作用，特别是拮抗剂活性的吡咯烷衍生物。更具体地，所述化合物在治疗和/或预防由氧催产素介导的疾病状态，包括早产、早产和痛经方面是有用的。本发明还涉及新型吡咯烷衍生物以及其制备方法，其中X从CR6R7、NOR6、NNR6R7组中选择；A从—(C═O)—、—(C═O)—O—、—C(═NH)—、—(C═O)—NH—、—(C═S)—NH、—SO22—、—SO2NH—、—CH2—中选择；B是一个群—(C═O)—NR8R9或表示具有式(a)的杂环残基，其中Q是NR10、O或S；n是选择的整数0、1或2；Y、Z和E与它们连接的2个碳一起形成一个5-6成员芳基或杂芳基环。
• S-5-SUBSTITUENT-N-2'-(THIOPHENE-2-YL)ETHYL-TETRALIN-2-AMINE OR CHIRAL ACID SALTS THEREOF AND USE FOR PREPARING ROTIGOTINE
  申请人：He Xungui

  公开号：US20130046100A1

  公开（公告）日：2013-02-21

  The chiral compound S-5-substituted-N-2′-(thienyl-2-yl-)ethyl-tetralin-2-amine or its chiral acid salts and preparation method thereof are disclosed, and the method for preparing Rotigotine by using the chiral compound is also disclosed. Racemic 5-substituted-N-2′-(thien-2-yl-)ethyl-tetralin-2-amine (compound 1) is resolved by using a conventional chiral acid to obtain an optically pure chiral acid salt of S-5-substituted-N-2′-(thien-2-yl-)ethyl-tetralin-2-amine, which is then dissociated to obtain S-5-substituted-N-2′-(thien-2-yl-)ethyl-tetralin-2-amine (compound 2). The compound 2 or chiral acid salt thereof is alkylated and deprotected to produce rotigotine (compound 5).

  所述的手性化合物S-5-取代-N-2′-(噻吩-2-基-)乙基-四氢萘-2-胺或其手性酸盐及其制备方法被揭示，并且还揭示了利用该手性化合物制备罗蒂果汀的方法。利用常规手性酸将混合物5-取代-N-2′-(噻吩-2-基-)乙基-四氢萘-2-胺（化合物1）分离，以获得S-5-取代-N-2′-(噻吩-2-基-)乙基-四氢萘-2-胺的光学纯手性酸盐，然后解离以获得S-5-取代-N-2′-(噻吩-2-基-)乙基-四氢萘-2-胺（化合物2）。化合物2或其手性酸盐经烷基化和去保护反应制备罗蒂果汀（化合物5）。
• Aminoacetamide acyl guanidines as beta-secretase inhibitors
  申请人：Gerritz Samuel

  公开号：US20060287287A1

  公开（公告）日：2006-12-21

  There is provided a series of substituted acyl guanidines of Formula (Ik) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R 2 , R 3 , R 4 , R 5 , R 25 , R 26 and R 27 as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

  提供了一系列的取代酰基胍类化合物，符合以下化学式（Ik）或其立体异构体；或其药学上可接受的盐，其中R2、R3、R4、R5、R25、R26和R27如本文所定义，它们的药物组合物和使用方法。这些化合物抑制β-分泌酶对淀粉样前体蛋白（APP）的加工，更具体地说，抑制Aβ肽的产生。本公开涉及对β-淀粉样蛋白产生相关的神经疾病的治疗有用的化合物，如阿尔茨海默氏病和其他受抗淀粉样活性影响的病症。
• DUAL-ACTING ANTIHYPERTENSIVE AGENTS
  申请人：Allegretti Paul

  公开号：US20090270473A1

  公开（公告）日：2009-10-29

  The invention relates to compounds having the formula: wherein: Q, W, Y, Z, r, and Ar are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT 1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

  这项发明涉及具有以下式的化合物：其中：Q、W、Y、Z、r 和 Ar 如规范中所定义，并其药学上可接受的盐。这些化合物具有AT1受体拮抗活性和酶抑制活性。该发明还涉及包含这些化合物的药物组合物；使用这些化合物的方法；以及制备这些化合物的过程和中间体。