2-bromo-5-(2-methoxyvinyl)pyridine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 2-bromo-5-(2-methoxyvinyl)pyridine
• 英文别名: 2-Bromo-5-(2-methoxy-vinyl)-pyridine；2-bromo-5-[(E)-2-methoxyethenyl]pyridine
• 化学式: C₈H₈BrNO
• 分子量: 214.062
• InChiKey: WQQGZZMDUMJLFO-SNAWJCMRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  22.1
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  甲氧基甲基三苯基氯化膦 、 2-溴-5-醛基吡啶 在 正丁基锂 作用下， 以 四氢呋喃 、 正己烷 为溶剂， 反应 16.0h， 生成 2-bromo-5-(2-methoxyvinyl)pyridine 、 2-bromo-5-(2-methoxyvinyl)pyridine
  参考文献：
  名称：

  在精神分裂症动物模型中具有功效的新型口服生物利用磷酸二酯酶10A（PDE10A）抑制剂的鉴定。

  摘要：

  我们报告继续重点医学化学计划，旨在进一步优化一系列咪唑并[1,2- a ]吡嗪类，作为一类新型的有效和选择性磷酸二酯酶10A（PDE10A）抑制剂。体外和体内药代动力学和药效学评估允许选择化合物25a在精神病的临床前模型中对其进行评估。描述了我们的药物化学程序的演变，结构-活性关系（SAR）分析以及优化的铅25a的详细药理特性。

  DOI：

  10.1021/jm501651a

文献信息

• [EN] IMIDAZO [1, 2 -A] PYRAZINE DERIVATIVES AND THEIR USE FOR THE PREVENTION OR TREATMENT OF NEUROLOGICAL, PSYCHIATRIC AND METABOLIC DISORDERS AND DISEASES<br/>[FR] DÉRIVÉS D'IMIDAZO[1,2-A]PYRAZINE ET LEUR UTILISATION POUR LA PRÉVENTION OU LE TRAITEMENT DE TROUBLES ET MALADIES NEUROLOGIQUES, PSYCHIATRIQUES ET MÉTABOLIQUES.
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2011110545A1

  公开（公告）日：2011-09-15

  The present invention relates to novel imidazo[1,2-a]pyrazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.

  本发明涉及新型咪唑并[1,2-a]吡嗪衍生物，它们是磷酸二酯酶10（PDE10）的抑制剂，并且对涉及PDE10酶的神经、精神和代谢性疾病的治疗或预防具有用处。该发明还涉及包含这类化合物的药物组合物，用于制备这类化合物和组合物的方法，以及利用这类化合物或药物组合物预防或治疗神经、精神和代谢性疾病和疾病。
• IMIDAZO[1,2-a]PYRAZINE DERIVATIVES AND THEIR USE FOR THE PREVENTION OR TREATMENT OF NEUROLOGICAL, PSYCHIATRIC AND METABOLIC DISORDERS AND DISEASES
  申请人：Bartolomé-Nebreda José Manuel

  公开号：US20120329792A1

  公开（公告）日：2012-12-27

  The present invention relates to novel imidazo[1,2-a]pyrazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.

  本发明涉及新型咪唑并[1,2-a]吡嗪衍生物，其为磷酸二酯酶10（PDE10）的抑制剂，并且适用于治疗或预防涉及PDE10酶的神经、精神和代谢性疾病。该发明还涉及包含这类化合物的药物组合物，制备这类化合物和组合物的方法，以及利用这类化合物或药物组合物预防或治疗神经、精神和代谢性疾病和疾病。
• Selective Estrogen Receptor Modulator
  申请人：Hamaoka Shinichi

  公开号：US20120004315A1

  公开（公告）日：2012-01-05

  The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like; formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; R a and R b are the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R′ represents 1 to 4 independent hydrogen atoms and the like; and R″ represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.

  本发明提供一种由以下式（I）表示的化合物; [其中T表示单键，可能具有取代基的C1-C4烷基和类似物；式（I-1）表示单键或双键；A表示单键，可能具有取代基的双价5-至14-成员杂环基和类似物；Y表示单键和类似物；Z表示亚甲基基团和类似物；环G表示苯基团和类似物，可能与5-至6-成员环缩合并可能具有杂原子；Ra和Rb相同或不同，表示氢原子和类似物；W表示单键和类似物；R'表示1到4个独立的氢原子和类似物；R''表示1到4个独立的氢原子和类似物]或其盐或水合物。
• Selective estrogen receptor modulator
  申请人：Hamaoka Shinichi

  公开号：US20060116364A1

  公开（公告）日：2006-06-01

  The present invention provides a compound represented by the following formula [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like; formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; R a and R b are the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R′ represents 1 to 4 independent hydrogen atoms and the like; and R″ represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof

  本发明提供了一种化合物，其表示为以下式子[其中T表示单键，C1-C4的烷基，可能带有取代基等；式(I-1)表示单键或双键；A表示单键，二价的5-至14-成员杂环基团，可能带有取代基等；Y表示单键等；Z表示亚甲基等；环G表示苯基团等，可与5-至6-成员环缩合并且可能具有杂原子；Ra和Rb相同或不同，表示氢原子等；W表示单键等；R'表示1至4个独立的氢原子等；R"表示1至4个独立的氢原子等]或其盐，或其水合物。
• SELECTIVE ESTROGEN RECEPTOR MODULATOR
  申请人：Hamaoka Shinichi

  公开号：US20090325930A1

  公开（公告）日：2009-12-31

  The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like; (I-1) formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; R a and R b are the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R′ represents 1 to 4 independent hydrogen atoms and the like; and R″ represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.

  本发明提供了一种由以下式（I）表示的化合物；[其中，T表示单键，C1-C4烷基，可以有取代基等；（I-1）式（I-1）表示单键或双键；A表示单键，双价的5-至14-成员杂环基，可以有取代基等；Y表示单键等；Z表示亚甲基等；环G表示苯基等，可以与5-至6-成员环缩合，可以有杂原子；Ra和Rb相同或不同，表示氢原子等；W表示单键等；R′表示1至4个独立的氢原子等；R″表示1至4个独立的氢原子等]或其盐，或其水合物。