2-aminobenzylphosphine | 54006-12-1

• 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: 2-aminobenzylphosphine
• 英文别名: 2-(Phosphanylmethyl)aniline
• CAS: 54006-12-1
• 化学式: C₇H₁₀NP
• 分子量: 139.137
• InChiKey: CCLCGVGMUYQVGQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  9
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  26
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  diethyl <(2-aminophenyl)methyl>phosphonate 在 lithium aluminium tetrahydride 作用下， 以 乙醚 为溶剂， 反应 3.0h， 以40%的产率得到2-aminobenzylphosphine
  参考文献：
  名称：

  A Tripodal Benzylene-Linked Trisamidophosphine Ligand Scaffold: Synthesis and Coordination Chemistry with Group(IV) Metals

  摘要：

  A new tripodal trisamidophosphine ligand (1) based on the trisbenzylphosphine backbone has been synthesized in three steps starting from NaPH2, and phthaloyl-protected 2-aminobenzyl bromide. At elevated temperatures, 1 reacts directly with M(NMe2)(4) (M = Zr, Hf) to afford the dimethylamido complexes [PN3]M(NMe2) (M = Zr, Hf) (2), which are easily converted into the corresponding triflates [PN3]MOTf (M = Zr, Hf) (3) via reaction with triethylsilyl trifluoromethanesulfonate. The related titanium chloro complex [PN3]TiCl (4-Ti) is obtained from 1 and Bn3TiCl via protonolysis. Triple deprotonation of 1 with n-butyllithium affords the tris-lithium salt Li-3[PN3] (1-Li), which serves as a common starting material for the preparation of all the group(IV) chlorides [PN3]MCl (M = Ti, Zr, Hf) (4). Upon treatment of 4-Ti with Bn2Mg(thf)(2), formation of a benzyltitanium species is observed, which is converted cleanly into a ligand-CH-activated species (5-Ti).

  DOI：

  10.1021/ic500163c

文献信息

• [EN] INDOLIC DERIVATIVES AND USE THEREOF IN MEDICAL FIELD<br/>[FR] DÉRIVÉS INDOLIQUES ET UTILISATION DE CELLES-CI DANS LE DOMAINE MÉDICAL
  申请人：UNI DEGLI STUDI DL ROMA LA SAPIENZA

  公开号：WO2011121629A1

  公开（公告）日：2011-10-06

  The present invention concerns indolic derivatives and use thereof in medical field. Particularly, the invention concerns 3-[(3',4',5'- trimethoxyphenyl)thio]-1 H-indole derivatives and bioisosteric derivatives thereof and their use for the treatment of tumours.

  本发明涉及吲哚衍生物及其在医学领域中的应用。具体而言，该发明涉及3-[(3',4',5'-三甲氧基苯基)硫基]-1 H-吲哚衍生物及其生物同位素衍生物，以及它们在肿瘤治疗中的应用。
• [EN] COMPOSITIONS AND METHODS USEFUL FOR TREATING DISEASES CHARACTERIZED BY INSUFFICIENT PANTOTHENATE KINASE ACTIVITY<br/>[FR] COMPOSITIONS ET MÉTHODES UTILES DANS LE TRAITEMENT DE MALADIES SE CARACTÉRISANT PAR UNE ACTIVITÉ INSUFFISANTE DE LA PANTOTHÉNATE KINASE
  申请人：ACIES BIO D O O

  公开号：WO2017218963A1

  公开（公告）日：2017-12-21

  Methods and pharmaceutical compositions for use in treating diseases associated with insufficient activity of the pantothenate kinase enzyme (e.g., CASTOR diseases) are disclosed. The methods and compositions involve an effective amount of an active derivative of 4'-phosphopantetheine.

  本发明揭示了用于治疗与泛酰胺激酶酶活性不足相关疾病（例如CASTOR疾病）的方法和药物组合物。这些方法和组合物涉及有效量的4'-磷酰泛酰胺的活性衍生物。
• 3-OXAZOLINONE COMPOUND, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL APPLICATION THEREOF
  申请人：Beijing InnoCare Pharma Tech Co., Ltd.

  公开号：EP3805212A1

  公开（公告）日：2021-04-14

  The present invention relates to a novel 3-indazolinone compound that regulates or inhibits the activity of indoleamine 2,3-dioxygenase (IDO), the method for the preparation thereof and the use thereof in medicine. In particular, the present invention relates to a compound represented by the general formula (I) and a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the compound or a pharmaceutically acceptable salt thereof, a method for treating or preventing IDO-mediated diseases, especially tumors, by use of the compound or a pharmaceutically acceptable salt thereof, and a method for preparing the compound or a pharmaceutically acceptable salt thereof. The present invention further relates to use of the compound or a pharmaceutically acceptable salt thereof or a composition comprising the compound or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for treating or preventing IDO-mediated diseases, especially tumors.Wherein the substituents of the general formula (I) are defined the same as that in the specification.

  本发明涉及一种调节或抑制吲哚胺-2,3-二氧化酶（IDO）活性的新型3-吲唑啉酮化合物、其制备方法及其在医学中的用途。特别是，本发明涉及通式（I）代表的化合物及其药学上可接受的盐、包含该化合物或其药学上可接受的盐的药物组合物、通过使用该化合物或其药学上可接受的盐治疗或预防IDO介导的疾病，特别是肿瘤的方法，以及制备该化合物或其药学上可接受的盐的方法。本发明进一步涉及该化合物或其药学上可接受的盐或包含该化合物或其药学上可接受的盐的组合物在制造治疗或预防IDO介导的疾病，特别是肿瘤的药物中的用途。其中通式（I）的取代基定义与说明书中的相同。