2-Ethyl-indolizin | 36766-60-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 英文名称: 2-Ethyl-indolizin
• 英文别名: 2-Ethyl-indolizine；2-ethylindolizine
• CAS: 36766-60-6
• 化学式: C₁₀H₁₁N
• 分子量: 145.204
• InChiKey: ZGNNFVXEWVYKRT-UHFFFAOYSA-N

物化性质

• 熔点：
  41 °C
• 沸点：
  128 °C(Press: 15 Torr)
• 密度：
  0.99±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  4.4
• 氢给体数：
  0
• 氢受体数：
  0

反应信息

• 作为反应物：
  描述：

  2-Ethyl-indolizin 以39%的产率得到
  参考文献：
  名称：

  ROSSEELS G.; INION H.; MATTEAZZI J.-R.; PEIREN M.; PROST M.; DESCAMPS M.;+, EUR. J. MED. CHEM., 1975, 10, NO 6, 579-584

  摘要：

  DOI：
• 作为产物：
  描述：

  1-<(ethoxycarbonyl)methyl>-2-picolinium chloride 以78%的产率得到
  参考文献：
  名称：

  ROSSEELS G.; INION H.; MATTEAZZI J.-R.; PEIREN M.; PROST M.; DESCAMPS M.;+, EUR. J. MED. CHEM., 1975, 10, NO 6, 579-584

  摘要：

  DOI：

文献信息

• A Practical Parallel Synthesis of 2-Substituted Indolizines
  作者：Wenying Chai、Annette Kwok、Victoria Wong、Nicholas I. Carruthers、Jiejun Wu

  DOI：10.1055/s-2003-42042

  日期：——

  A practical parallel synthesis of 2-substituted indolizines 4 via phase-separation techniques is reported. Their further transformation into indolizidines 5 is also described.

  报告了一种通过相分离技术实现的2-取代吲唑啉4的实用并行合成方法，并描述了它们进一步转化为吲唑啶5的过程。
• Indolizine derivatives and uses in therapeutics
  申请人：S. A. Labaz-Sanofi N.V.

  公开号：US04400387A1

  公开（公告）日：1983-08-23

  Indolizine derivatives represented by the general formula: ##STR1## wherein R represents a straight- or branched-chain alkyl radical having from 1 to 8 carbon atoms, or a phenyl group non-substituted or bearing one or two substituents, which may be the same or different, selected from halogen atoms, for example fluorine, chlorine and bromine and from lower alkyl and alkoxy groups, for example methyl and methoxy and X.sub.1, X.sub.2 and X.sub.3, which may be the same or different, each represent hydrogen, chlorine, bromine or methoxy with the proviso that when they are identical X.sub.1, X.sub.2 and X.sub.3 are not simultaneously hydrogen. They possess an inhibitory activity with respect to the action of xanthine oxidase and of adenosine deaminase as well as an uricosuric action and can be used in the treatment of physiological disturbances consequent upon an excess of uric acid, upon disorders of the immunization system and as antiparasitic agents.

  印度利津衍生物的一般化学式为：##STR1##其中R代表具有1至8个碳原子的直链或支链烷基基团，或者是一个非取代的苯基团或带有一个或两个取代基，这些取代基可以是相同的也可以是不同的，选择自卤素原子，例如氟、氯和溴，以及较低的烷基和烷氧基团，例如甲基和甲氧基，以及X.sub.1、X.sub.2和X.sub.3，这些可以是相同的也可以是不同的，每个代表氢、氯、溴或甲氧基，但当它们相同时，X.sub.1、X.sub.2和X.sub.3不能同时为氢。它们具有对黄嘌呤氧化酶和腺苷脱氨酶的抑制活性，以及尿酸排泄作用，可用于治疗由尿酸过多引起的生理紊乱，免疫系统紊乱和作为抗寄生虫剂。
• Indolizine derivatives, pharmaceutical compositions and methods
  申请人：Labaz

  公开号：US04103012A1

  公开（公告）日：1978-07-25

  Novel indolizine derivatives of the general formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, wherein R represents a branched- or straight-chain alkyl radical having from 1 to 5 carbon atoms, a phenyl radical, a mono-fluoro-, mono-chloro- or mono-bromo-phenyl, a di-fluoro-, di-chloro- or di-bromo-phenyl radical, a methoxy-phenyl radical or a methyl-phenyl radical optionally substituted on the aromatic moiety by an atom of fluorine, chlorine or bromine and R.sub.1 and R.sub.2, which are different, represent a hydrogen atom or a group of the formula: ##STR2## wherein R.sub.3 and R.sub.4 which are identical, each represent a hydrogen atom or a methyl radical, Am represents a dimethylamino, diethylamino, di-n-propylamino, di-n-butylamino, morpholino, piperidino, pyrrolidino or 4-methyl-piperazino group and n is an integer in the range of from 2 to 6 inclusive. They are effective for treating certain pathological or otherwise abnormal conditions of the heart and more particularly sinus tachycardia. Certain of them are also useful in the treatment of angina pectoris and cardiac arrhythmia.

  新型的吲哚啉衍生物具有一般式：##STR1##及其药用可接受的酸盐，其中R代表具有1至5个碳原子的支链或直链烷基基团，苯基，单氟，单氯或单溴苯基，二氟，二氯或二溴苯基，甲氧基苯基或甲基苯基，其在芳香基上可选择地被氟，氯或溴原子取代，而R.sub.1和R.sub.2，它们不同，代表氢原子或具有以下式的基团：##STR2##其中R.sub.3和R.sub.4相同，各代表氢原子或甲基基团，Am代表二甲胺，二乙胺，二正丙胺，二正丁胺，吗啉，哌啶，吡咯啉或4-甲基哌嗪基团，n为在2至6之间的整数。它们有效用于治疗心脏的某些病理性或其他异常情况，尤其是窦性心动过速。其中一些也可用于治疗心绞痛和心律失常。
• NOVEL INDOLIZINE DERIVATIVES, METHOD FOR PREPARING SAME, AND THERAPEUTIC COMPOSITIONS COMPRISING SAME
  申请人：GAUTIER Patrick

  公开号：US20080287485A1

  公开（公告）日：2008-11-20

  The present invention is directed to compounds of formula (I): described as novel indolizine derivatives and to a method for their preparation along with pharmaceutical compositions thereof whose substituents are as described in the specification.

  本发明涉及公式(I)的化合物，被描述为新颖的吲哚啉衍生物，以及它们的制备方法和所述规范中描述的药用组合物。
• PYRIDAZINONES, METHOD OF MAKING, AND METHOD OF USE THEREOF
  申请人：Barbosa JR. Antonio J.M.

  公开号：US20110301145A1

  公开（公告）日：2011-12-08

  Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.

  本文描述了化学式I的化合物，其能够抑制Btk。本文还描述了包含至少一种化学式I化合物的制药组合物，以及至少选择自载体、佐剂和赋形剂中的一种药学可接受载体的制药组合物。本文还描述了治疗对Btk活性和/或B细胞活性抑制有响应的某些疾病的患者的方法。本文还描述了检测样品中Btk存在的方法。