2(1H)-异喹啉甲醛 | 208348-23-6

• 分子结构分类: 有机化合物 - 苯类化合物
• 中文名称: 2(1H)-异喹啉甲醛
• 英文名称: 2-formyl-1,2-dihydroisoquinoline
• 英文别名: isoquinoline-2(1H)-carbaldehyde；isoquinoline-2-carboxaldehyde；1H-isoquinoline-2-carbaldehyde
• CAS: 208348-23-6
• 化学式: C₁₀H₉NO
• 分子量: 159.188
• InChiKey: RKIQWXMIFPFQFP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  异喹啉 、 formamide 反应 4.0h， 以7%的产率得到2(1H)-异喹啉甲醛
  参考文献：
  名称：

  Reductive Formylation of Isoquinoline Derivatives with Formamide and Synthesis of 2-Formyltetrahydroisoquinolines

  摘要：

  Reductive formylation of isoquinoline derivatives as 3,4-dihydroisoquinolines 1, enamines and enamides of tetrahydroisoquinoline 2 and the reaction of 2-(2-acylphenyl)ethylamides 3 with formamide afforded the corresponding N-formyltetrahydroisoquinolines 4 and N-acyltetrahydroisoquinolines 5.

  DOI：

  10.1080/00397919808006842

文献信息

• [EN] 1,1'-DIADAMANTYL CARBOXYLIC ACIDS, MEDICAMENTS CONTAINING SUCH COMPOUNDS AND THEIR USE<br/>[FR] ACIDES 1,1'-DIADAMANTYL CARBOXYLIQUES, MÉDICAMENTS CONTENANT DE TELS COMPOSÉS ET APPLICATION ASSOCIÉE
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2010010174A1

  公开（公告）日：2010-01-28

  The present invention relates to compounds defined by formula (I) wherein the group R is defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases.

  本发明涉及由式（I）定义的化合物，其中基团R如权利要求1中所定义，具有有价值的药理活性。特别是这些化合物是11β-羟基类固醇脱氢酶（HSD）1的抑制剂，因此适用于治疗和预防可以受到该酶抑制影响的疾病，如代谢性疾病。
• [EN] SUBSTITUTED N-ALKYL AND N-ACYL TETRAHYDRO-ISOQUINOLINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF<br/>[FR] DÉRIVÉS N-ALKYL ET N-ACYL TÉTRAHYDRO-ISOQUINOLINE SUBSTITUÉS, PROCÉDÉ DE PRÉPARATION ET APPLICATION THÉRAPEUTIQUES ASSOCIÉS
  申请人：SANOFI SA

  公开号：WO2011143145A1

  公开（公告）日：2011-11-17

  The present invention discloses and claims a series of substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives of formula (I). Wherein R, R1, R2, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives of formula (I) and intermediates therefor.

  本发明揭示并声明了一系列式(I)的取代N-烷基和N-酰基四氢异喹啉衍生物。其中R、R1、R2、X、m、n和p如本文所述。更具体地，本发明的化合物是H3受体的调节剂，因此在制药剂中特别有用，尤其是在治疗和/或预防由H3受体调节的各种疾病，包括与中枢神经系统相关的疾病。此外，本发明还揭示了制备式(I)的取代N-烷基和N-酰基四氢异喹啉衍生物及其中间体的方法。
• KETOLIDE DERIVATIVES AS ANTIBACTERIAL AGENTS
  申请人：Das Biswajit

  公开号：US20090170790A1

  公开（公告）日：2009-07-02

  The present invention provides ketolide derivatives, which can be used as anti-bacterial agents. Compounds disclosed herein can be used for the treating or preventing conditions caused by or contributed to by gram positive, gram negative or anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Moraxalla spp., Chlamydia spp., Mycoplasm, Legionella spp., Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Bacillus , Enterobactericeae or any combination thereof. Also provided are processes for preparing compounds disclosed herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods of treating bacterial infections.

  本发明提供了酮烯类衍生物，可用作抗菌剂。本文披露的化合物可用于治疗或预防由革兰氏阳性、革兰氏阴性或厌氧细菌引起或导致的疾病，更具体地针对例如葡萄球菌、链球菌、肠球菌、流感嗜血杆菌、嗜痰菌属、衣原体属、支原体、军团菌属、分枝杆菌、幽门螺杆菌、梭菌、拟杆菌、白色杆菌、杆菌、肠杆菌科细菌或其任意组合。还提供了制备本文披露的化合物的方法、用于合成的中间体、其制药组合物以及治疗细菌感染的方法。
• [EN] PROCESS FOR THE PREPARATION OF AN ENANTIOMERICALLY PURE TRISUBSTITUTED 1,2,3,4-TETRAHYDROISOQUINOLINE DERIVATIVE<br/>[FR] PROCÉDÉ POUR LA PRÉPARATION D'UN DÉRIVÉ TRISUBSTITUÉ ÉNANTIOMÉRIQUEMENT PUR DE LA 1,2,3,4-TÉTRAHYDROISOQUINOLINE
  申请人：ACTELION PHARMACEUTICALS LTD

  公开号：WO2011001373A1

  公开（公告）日：2011-01-06

  The present invention relates to a process for the preparation of the compound of formula 7, which process comprises: the asymmetric transfer hydrogenation of the compound of formula 4 * HX: wherein HX is as decribed in the description; in the presence of an optically active Noyori- type transfer hydrogenation catalyst, at a substrate to catalyst ratio of more than 100:1 mol equivalent; a reducing agent; and a solvent; to obtain the compound of formula 7.

  本发明涉及制备式7化合物的过程，该过程包括：在具有光学活性的Noyori型转移氢化催化剂的存在下，以底物与催化剂比大于100:1摩尔当量的条件下，使用还原剂和溶剂进行式4* HX化合物的不对称转移氢化反应，以获得式7化合物。其中HX如说明中所述。
• Pyrroloisoquinolines
  申请人：MAY & BAKER LIMITED

  公开号：EP0303446A1

  公开（公告）日：1989-02-15

  Pyrrolo[2,1-a]isoquinoline derivatives of the formula: wherein R¹ and R² each represent cycloalkyl or alkyl, alkenyl or alkynyl which may be halogen-substituted, or optionally substituted aryl or heteroaryl, X represents ethylene or vinylene, R³ represents a group of the formula: -Y-CH₂-CH(OH)-CH₂-COOR⁵      II wherein Y represents carbonyl or hydroxymethylene and R⁵ represents hydrogen or optionally substituted alkyl, or R³ represents a lactone ring, and the symbols R⁴ represent hydrogen, halogen, optionally substituted alkyl, alkenyl or alkynyl, optionally substituted aryl or heteroaryl, or a group of the formula R⁶O-, wherein R⁶ represents alkyl, aryl or arylalkyl have useful pharmaceutical properties.

  式中的吡咯并[2,1-a]异喹啉衍生物： 其中 R¹ 和 R² 各自代表环烷基或可被卤素取代的烷基、烯基或炔基，或任选取代的芳基或杂芳基，X 代表乙烯或乙烯基，R³ 代表式中的一个基团： -Y-CH₂-CH（OH）-CH₂-COOR⁵ II 其中 Y 代表羰基或羟甲基，R⁵ 代表氢或任选取代的烷基，或 R³ 代表内酯环，符号 R⁴ 代表氢、卤素、任选取代的烷基、烯基或炔基、任选取代的芳基或杂芳基，或式 R⁶O- 的基团，其中 R⁶ 代表烷基、芳基或芳基烷基。