雷克西米诺 | 52883-35-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 雷克西米诺
• 英文名称: 2-Imino-4-phenyloxazolidin
• 英文别名: 4-phenyl-4,5-dihydro-oxazol-2-ylamine；Rexamino；4-phenyl-4,5-dihydro-1,3-oxazol-2-amine
• CAS: 52883-35-9
• 化学式: C₉H₁₀N₂O
• mdl: MFCD18382428
• 分子量: 162.191
• InChiKey: ZBFPLELNWIASCT-UHFFFAOYSA-N

物化性质

• 溶解度：
  可溶于氯仿（少许）、甲醇（少许）

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.222
• 拓扑面积：
  47.6
• 氢给体数：
  1
• 氢受体数：
  2

安全信息

• 海关编码：
  2934999090

反应信息

• 作为反应物：
  描述：

  雷克西米诺 以53%的产率得到
  参考文献：
  名称：

  TANAKA CHIAKI; OGATA IKUTOSHI; NISHIDA MOTONOBU, YAKUGAKU DZASSI, YAKUGAKU ZASSNI, J. PHARM. SOS. JAR., 1977, 97, NO 2, 15+

  摘要：

  DOI：
• 作为产物：
  描述：

  苯乙烯 、 氰胺 在 phenylselenenyl sulfate 作用下， 以 1,4-二氧六环 、 水 为溶剂， 反应 23.0h， 以54%的产率得到雷克西米诺
  参考文献：
  名称：

  One-Pot Conversion of Alkenes into Oxazolines and Oxazolidin-2-Ones Promoted by Diphenyl Diselenide

  摘要：

  Oxazolines or oxazolidin-2-ones are produced from the reaction of diphenyl diselenide, ammonium persulfate and trifluoromethanesulfonic acid with alkenes in the presence of MeCN/H2O, NH2CN/H2O or NH2CO2Et.

  DOI：

  10.1080/00397919708005461

文献信息

• [EN] AZITHROMYCIN ANTIMICROBIAL DERIVATIVES WITH NON-ANTIBIOTIC PHARMACEUTICAL EFFECT<br/>[FR] DÉRIVÉS ANTIMICROBIENS D'AZITHROMYCINE À EFFET PHARMACEUTIQUE NON ANTIBIOTIQUE
  申请人：PROBIOTIC PHARMACEUTICALS APS

  公开号：WO2014166503A1

  公开（公告）日：2014-10-16

  The invention provides molecules, which are based on a modification of azithromycin, removing the antibiotic effect, while retaining other beneficial effects, such as, but not limited to imunomodulatory effects. The compounds of the invention can be described by compounds of Formula (I) as further defined herein.

  该发明提供了一种分子，该分子基于对阿奇霉素的修改，去除了抗生素效应，同时保留了其他有益效果，比如但不限于免疫调节效应。该发明的化合物可通过以下公式(I)定义的化合物来描述。
• OXAZOLINE DERIVATIVES
  申请人：Galley Guido

  公开号：US20110112080A1

  公开（公告）日：2011-05-12

  The invention relates to compounds of formula I wherein the definitions of X, R and R 1 are as defined herein. The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.

  该发明涉及公式I中的化合物，其中X、R和R1的定义如本文所述。公式I中的化合物对痕量胺相关受体（TAARs）有良好的亲和力，特别是对TAAR1。这些化合物可用于治疗抑郁症、焦虑障碍、躁郁症、注意力缺陷多动障碍（ADHD）、与压力相关的障碍、精神分裂症等精神障碍、帕金森病等神经疾病、阿尔茨海默病等神经退行性疾病、癫痫、偏头痛、高血压、物质滥用和代谢性障碍，如进食障碍、糖尿病、糖尿病并发症、肥胖、血脂异常、能量消耗和吸收障碍、体温稳态障碍、睡眠和昼夜节律障碍以及心血管疾病。
• 2-Aminooxazolines as TAAR1 ligands
  申请人：Galley Guido

  公开号：US20080261920A1

  公开（公告）日：2008-10-23

  The invention relates to compounds of formula I wherein X, Y, R 1 , R 2 , and n are as defined herein or to a pharmaceutically suitable acid addition salt thereof. The invention also relates to pharmaceutical compositions containing such compounds and methods for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases include depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.

  本发明涉及化合物I的公式，其中X，Y，R1，R2和n如本文所定义，或其药学上适宜的酸加盐。本发明还涉及含有这种化合物的制药组合物和治疗与微量胺相关受体的生物学功能相关的疾病的方法，这些疾病包括抑郁症、焦虑症、双相情感障碍、注意力缺陷多动障碍、压力相关障碍、精神障碍、精神分裂症、神经系统疾病、帕金森病、神经退行性疾病、阿尔茨海默病、癫痫、偏头痛、物质滥用和代谢性疾病、进食障碍、糖尿病、糖尿病并发症、肥胖症、血脂异常、能量消耗和吸收障碍、体温稳态障碍和功能障碍、睡眠和昼夜节律障碍以及心血管疾病。
• 2-AMINOOXAZOLINES AS TAAR1 LIGANDS
  申请人：Galley Guido

  公开号：US20100120864A1

  公开（公告）日：2010-05-13

  The invention relates to compounds of formula I wherein X, Y, R 1 , R 2 , and n are as defined herein or to a pharmaceutically suitable acid addition salt thereof. The invention also relates to pharmaceutical compositions containing such compounds and methods for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases include depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.

  本发明涉及式I的化合物，其中X，Y，R1，R2和n如本文所定义，或其药学适宜的酸加盐。本发明还涉及含有此类化合物的制药组合物，以及用于治疗与微量胺相关受体的生物学功能相关的疾病的方法，这些疾病包括抑郁症，焦虑症，双相情感障碍，注意力缺陷多动障碍，应激相关障碍，精神疾病，精神分裂症，神经疾病，帕金森病，神经退行性疾病，阿尔茨海默病，癫痫，偏头痛，物质滥用和代谢性疾病，进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和吸收障碍，体温稳态障碍和功能障碍，睡眠和生物钟节律障碍以及心血管疾病。
• An Efficient Synthesis of a New Series of Acyclonucleosides Starting from β-Amino Alcohols
  作者：Claude Agami、Luc Dechoux、Louis Hamon、Mohand Melaimi

  DOI：10.1021/jo000812d

  日期：2000.10.1

  A series of new acyclonucleosides analogues 3 has been synthesized very efficiently in three steps starting from beta-amino alcohols 1. The key step of this process is a nucleophilic substitution with various nucleophiles on 2,2'-anhydronucleosides 2. The chemo- and stereoselectivities of this reaction are discussed. AM1 calculations sustained the observed chemoselectivity.