四氢糠酰哌嗪 氢溴酸盐 | 63590-62-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 中文名称: 四氢糠酰哌嗪 氢溴酸盐
• 中文别名: 四氢糠酰哌嗪氢溴酸盐；N-(2-四氢呋喃甲酰基)哌嗪氢溴酸盐；1-(2-四氢呋喃甲酰基)哌嗪氢溴酸盐
• 英文名称: 1-[[(2RS)-2,3,4,5-tetrahydrofuran-2-yl]carbonyl]piperazine hydrobromide
• 英文别名: N-[2-tetrahydrofuroyl]piperazine hydrobromide；tetrahydrofuroyl piperazine HBr；(RS)-1-[[2,3,4,5-tetrahydrofuran-2-yl]carbonyl]piperazine hydrobromide；1-(2-Tetrahydrofuroyl)piperazine hydrobromide；oxolan-2-yl(piperazin-1-yl)methanone;hydrobromide
• CAS: 63590-62-5
• 化学式: BrH*C₉H₁₆N₂O₂
• mdl: MFCD03701619
• 分子量: 265.15
• InChiKey: IMMDGWNBMNOMPW-UHFFFAOYSA-N

物化性质

• 熔点：
  103-107 °C(lit.)
• 稳定性/保质期：

  遵照规定使用和储存，则不会分解。

计算性质

• 辛醇/水分配系数(LogP)：
  -0.68
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.888
• 拓扑面积：
  41.6
• 氢给体数：
  2
• 氢受体数：
  3

安全信息

• 危险品标志：
  Xi
• 危险类别码：
  R36/37/38
• WGK Germany：
  3
• 海关编码：
  2934999090
• 安全说明：
  S26,S36
• 危险标志：
  GHS07
• 危险性描述：
  H315,H319,H335
• 危险性防范说明：
  P261,P305 + P351 + P338

制备方法与用途

用途：用作盐酸特拉唑嗪的中间体

反应信息

• 作为反应物：
  描述：

  四氢糠酰哌嗪 氢溴酸盐 、 2-氯-4-氨基-6,7-二甲氧基喹唑啉 在 三乙胺 作用下， 以 正丁醇 为溶剂， 反应 3.0h， 生成 1-(4-amino-6,7-dimethoxyquinazolin-2-yl)-4-[[(2RS)2,3,4,5-tetrahydrofuran-2-yl]carbonyl]piperazine hydrochloride hydrobromide
  参考文献：
  名称：

  Process for the preparation of terazosin hydrocloride dihydrate

  摘要：

  本发明涉及一种改进的制备方法，用于制备式I的1-(4-氨基-6,7-二甲氧基喹唑啉-2-基)-4-[[（2RS）-2,3,4,5-四氢呋喃-2-基]羰基]哌嗪盐酸盐二水合物，通过中间体1-(4-氨基-6,7-二甲氧基喹唑啉-2-基)-4-[[（2RS）-2,3,4,5-四氢呋喃-2-基]羰基]哌嗪盐酸盐/溴化物(V)。

  公开号：

  US20070161791A1
• 作为产物：
  描述：

  四氢糠酰哌嗪 在 氢溴酸 作用下， 以 水 、 正丁醇 为溶剂， 反应 1.5h， 生成 四氢糠酰哌嗪 氢溴酸盐
  参考文献：
  名称：

  Process for the preparation of terazosin hydrocloride dihydrate

  摘要：

  本发明涉及一种改进的制备方法，用于制备式I的1-(4-氨基-6,7-二甲氧基喹唑啉-2-基)-4-[[（2RS）-2,3,4,5-四氢呋喃-2-基]羰基]哌嗪盐酸盐二水合物，通过中间体1-(4-氨基-6,7-二甲氧基喹唑啉-2-基)-4-[[（2RS）-2,3,4,5-四氢呋喃-2-基]羰基]哌嗪盐酸盐/溴化物(V)。

  公开号：

  US20070161791A1

文献信息

• [EN] INDAZOLE-CARBOXAMIDE COMPOUNDS AS 5-HT4 RECEPTOR AGONISTS<br/>[FR] COMPOSÉS D'INDAZOLE-CARBOXAMIDE EN TANT QU'AGONISTES DE RÉCEPTEUR 5-HT4
  申请人：THERAVANCE INC

  公开号：WO2005080389A1

  公开（公告）日：2005-09-01

  The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.

  这项发明提供了新型吲唑基-羧酰胺5-HT4受体激动剂化合物。该发明还提供了包含这些化合物的药物组合物，使用这些化合物治疗与5-HT4受体活性相关的疾病的方法，以及用于制备这些化合物的过程和中间体。
• Use of .alpha..sub.1C specific compounds to treat benign prostatic
  申请人：Synaptic Pharmaceutical Corporation

  公开号：US05403847A1

  公开（公告）日：1995-04-04

  A method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound which binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity greater than ten-fold higher than the binding affinity with which the compound binds to a human .alpha..sub.1A adrenergic receptor, a human .alpha..sub.1B adrenergic receptor, and a human histamine H.sub.1 receptor, and, binds to a human .alpha..sub.2 adrenergic receptor with a binding affinity which is greater than ten-fold lower than the binding affinity with which the compound binds to such .alpha..sub.1C adrenergic receptor. Compounds meeting these criteria are provided.

  一种治疗良性前列腺增生症的方法，包括向受试者施用一种治疗有效量的化合物，该化合物与人类α1C肾上腺素能受体结合的结合亲和力比其与人类α1A肾上腺素能受体、人类α1B肾上腺素能受体和人类组胺H1受体结合的结合亲和力高出十倍以上，并且与人类α2肾上腺素能受体的结合亲和力比其与此类α1C肾上腺素能受体结合的结合亲和力低出十倍以上。提供了符合这些标准的化合物。
• USE OF ALPHA-1C SPECIFIC COMPOUNDS TO TREAT BENIGN PROSTATIC HYPERPLASIA
  申请人：——

  公开号：US20020032219A1

  公开（公告）日：2002-03-14

  A method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound which binds to a human &agr; 1C adrenergic receptor with a binding affinity greater than ten-fold higher than the binding affinity with which the compound binds to a human &agr; 1A adrenergic receptor, a human &agr; 1B adrenergic receptor, and a human histamine H 1 receptor, and, binds to a human &agr; 2 adrenergic receptor with a binding affinity which is greater than ten-fold lower than the binding affinity with which the compound binds to such &agr; 1C adrenergic receptor. Compounds meeting these criteria are provided.

  一种治疗良性前列腺增生症的方法，包括向患者施用一种治疗有效量的化合物，该化合物与人类α1C肾上腺素受体结合的亲和力比其与人类α1A肾上腺素受体、人类α1B肾上腺素受体和人类组胺H1受体结合的亲和力高出十倍以上，并且与人类α2肾上腺素受体结合的亲和力比其与α1C肾上腺素受体结合的亲和力低十倍以上。提供符合这些标准的化合物。
• Compositions comprising alpha-1C specific compounds
  申请人：Synaptic Pharmaceutical Corporation

  公开号：US20030022900A1

  公开（公告）日：2003-01-30

  A method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound which binds to a human &agr; 1C adrenergic receptor with a binding affinity greater than ten-fold higher than the binding affinity with which the compound binds to a human &agr; 1A adrenergic receptor, a human &agr; 1B adrenergic receptor, and a human histamine H 1 receptor, and, binds to a human &agr; 2 adrenergic receptor with a binding affinity which is greater than ten-fold lower than the binding affinity with which the compound binds to such &agr; 1C adrenergic receptor. Compounds meeting these criteria are provided.

  一种治疗良性前列腺增生的方法，包括向患者施用一种与人类α1C肾上腺素能受体结合的化合物，其结合亲和力比其与人类α1A肾上腺素能受体、人类α1B肾上腺素能受体和人类组胺H1受体结合的亲和力高出十倍以上，并且与人类α2肾上腺素能受体的结合亲和力比其与该α1C肾上腺素能受体结合的亲和力低十倍以上。提供了符合这些标准的化合物。
• Aromatic amine derivatives
  申请人：Synaptic Pharmaceutical Corporation

  公开号：US05508306A1

  公开（公告）日：1996-04-16

  This invention relates to novel aromatic amine compounds having the structure: ##STR1## where each W, Z.sup.1 and Z.sup.2 is independently H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, OH, F, Cl, Br, I, NO.sub.2, CN, SO.sub.2 NHR.sup.3, NR.sup.4.sub.2, CONR.sup.3.sub.2, COR.sup.5 ; where each R.sup.1 and R.sup.2 is independently H, C.sub.1 -C.sub.6 straight or branched chain alkyl or phenyl; where each X and Y is independently CH.sub.2, NR.sup.4, S, S.dbd.O, SO.sub.2 ; where n is 0, 1 or 2; where each p and q is independently 1 or 2; where R.sup.3 is H, C.sub.1 -C.sub.6 straight or branched chain alkyl or phenyl; where R.sup.4 is H, C.sub.1 -C.sub.6 straight or branched chain alkyl or COR.sup.3 ; and where R.sup.5 is H, C.sub.1 -C.sub.6 straight or branched chain alkyl or phenyl, C.sub.1 -C.sub.6 straight or branched chain alkoxy or OH. In addition the invention includes using such compounds for the treatment of benign prostatic hyperplasia, lowering intraocular pressure and inhibiting cholesterol synthesis.

  本发明涉及具有以下结构的新型芳香胺化合物：##STR1## 其中每个W，Z.sup.1和Z.sup.2独立地为H，C.sub.1-C.sub.6烷基，C.sub.1-C.sub.6烷氧基，OH，F，Cl，Br，I，NO.sub.2，CN，SO.sub.2NHR.sup.3，NR.sup.4.sub.2，CONR.sup.3.sub.2，COR.sup.5；其中每个R.sup.1和R.sup.2独立地为H，C.sub.1-C.sub.6直链或支链烷基或苯基；其中每个X和Y独立地为CH.sub.2，NR.sup.4，S，S.dbd.O，SO.sub.2；其中n为0、1或2；其中每个p和q独立地为1或2；其中R.sup.3为H，C.sub.1-C.sub.6直链或支链烷基或苯基；其中R.sup.4为H，C.sub.1-C.sub.6直链或支链烷基或COR.sup.3；其中R.sup.5为H，C.sub.1-C.sub.6直链或支链烷基或苯基，C.sub.1-C.sub.6直链或支链烷氧基或OH。此外，本发明还包括使用这些化合物治疗良性前列腺增生、降低眼压和抑制胆固醇合成。