4-aminobutan-2-ol tosylate

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4-aminobutan-2-ol tosylate
• 英文别名: 4-Aminobutan-2-yl 4-methylbenzenesulfonate
• 化学式: C₁₁H₁₇NO₃S
• 分子量: 243.327
• InChiKey: AJWXAOUYMIALQM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  16
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  77.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  对甲苯磺酸 、 4-氨基-2-丁醇 以 乙醇 为溶剂， 反应 6.0h， 以0.85 g的产率得到4-aminobutan-2-ol tosylate
  参考文献：
  名称：

  1-烯基膦酰胺酸二乙酯的新途径

  摘要：

  已经研究了由可烯醇化的羰基化合物衍生的N-（二乙氧基磷酰基）亚胺的新途径。研究了三种不同的方法：（i）乙基-[ N-（二乙氧基磷酰基）]-甲酰亚胺的氮杂-克莱森缩合与可烯醇化的酮；（ii）N-亚磺酰基磷酸氨基二乙酯与脂肪族醛之间的反应；以及（iii）热裂解诱导的氨基磷酸二乙酯与酮二乙缩醛的反应。除两种情况外，所有产物均被鉴定为1-烯基膦酸二乙酯，在光谱上检测不到亚胺互变异构体。可以推荐将氮杂-克莱森缩合反应作为一种简单有效的方法，以合成1-乙基烯基-3-氧代膦酸二乙酯。

  DOI：

  10.1016/s0040-4020(00)00568-8

文献信息

• [EN] INDOLE AND BENZOMORPHOLINE DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS<br/>[FR] DÉRIVÉS D'INDOLE ET DE BENZOMORPHOLINE EN TANT QUE MODULATEURS DES RÉCEPTEURS MÉTABOTROPIQUES DU GLUTAMATE
  申请人：ORTHO MCNEIL JANSSEN PHARM

  公开号：WO2010043396A1

  公开（公告）日：2010-04-22

  The present invention relates to novel compounds, in particular novel indole and benzomorpholine derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors - subtype 2 ("mGluR2") which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

  本发明涉及新颖化合物，特别是根据式(I)的新型吲哚和苯并吗啡啉衍生物，其中所有基团如申请和索赔中所定义。根据本发明的化合物是代谢型受体-亚型2（"mGluR2"）的阳性变构调节剂，对于治疗或预防与谷氨酸功能障碍相关的神经和精神障碍以及涉及代谢型受体中mGluR2亚型的疾病是有用的。特别是，这些疾病是来自焦虑、精神分裂症、偏头痛、抑郁症和癫痫的中枢神经系统疾病。该发明还涉及制备这种化合物和组合物的药物组合物和过程，以及利用这种化合物预防和治疗涉及mGluR2的这些疾病。
• INDOLE AND BENZOMORPHOLINE DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
  申请人：Cid-Nunez Jose Maria

  公开号：US20110275624A1

  公开（公告）日：2011-11-10

  The present invention relates to novel compounds, in particular novel indole and benzomorpholine derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

  本发明涉及一种新型化合物，特别是根据公式（I）中定义的所有基团的新型吲哚和苯并吗啡衍生物。本发明的化合物是代谢型受体亚型2（“mGluR2”）的正向变构调节剂，可用于治疗或预防与谷氨酸功能障碍有关的神经和精神障碍以及涉及代谢型受体亚型2的疾病。特别是，这些疾病是从焦虑、精神分裂症、偏头痛、抑郁症和癫痫等中枢神经系统疾病中选择的。本发明还涉及制备这种化合物和组合物的制药组合物和制备过程，以及使用这种化合物预防和治疗涉及mGluR2的这些疾病。
• New Routes to Diethyl 1-Alkenylphosphoramidates
  作者：Anna Napieraj、Stefan Zawadzki、Andrzej Zwierzak

  DOI：10.1016/s0040-4020(00)00568-8

  日期：2000.8

  )imines derived from enolizable carbonyl compounds have been investigated. Three different procedures were studied: (i) the aza-Claisen condensation of ethyl-[N-(diethoxyphosphoryl)]-formimidate with enolizable ketones, (ii) the reaction between diethyl N-sulfinylphosphoramidate and aliphatic aldehydes, and (iii) the thermally induced reaction of diethyl phosphoramidate with ketone diethyl acetals

  已经研究了由可烯醇化的羰基化合物衍生的N-（二乙氧基磷酰基）亚胺的新途径。研究了三种不同的方法：（i）乙基-[ N-（二乙氧基磷酰基）]-甲酰亚胺的氮杂-克莱森缩合与可烯醇化的酮；（ii）N-亚磺酰基磷酸氨基二乙酯与脂肪族醛之间的反应；以及（iii）热裂解诱导的氨基磷酸二乙酯与酮二乙缩醛的反应。除两种情况外，所有产物均被鉴定为1-烯基膦酸二乙酯，在光谱上检测不到亚胺互变异构体。可以推荐将氮杂-克莱森缩合反应作为一种简单有效的方法，以合成1-乙基烯基-3-氧代膦酸二乙酯。