2-tert-butyl-oxazoline | 30393-80-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑啉类
• 英文名称: 2-tert-butyl-oxazoline
• 英文别名: 2-tert.-Butyl-Δ²-oxazolin；2-t-Butyl-oxazolin；2-tert-butyl-4,5-dihydro-oxazole；2-t-Butyl-2-oxazoline；2-tert-butyl-4,5-dihydro-1,3-oxazole
• CAS: 30393-80-7
• 化学式: C₇H₁₃NO
• 分子量: 127.186
• InChiKey: ZEBDQSMWXLUBOI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  9
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  21.6
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  methyl 3-((tert-butyldimethylsilyl)oxy)-2-diazopent-3-enoate 、 2-tert-butyl-oxazoline 在 silver hexafluoroantimonate 作用下， 以 氯仿 为溶剂， 以81%的产率得到
  参考文献：
  名称：

  烯醇重氮乙酸酯和亚氨基醚的 AgI 催化反应：高度官能化吡咯的合成

  摘要：

  报道了一种前所未有的 Ag I催化有效方法，用于通过 [3+2]-环加成/C-O 键裂解/[1,5]-质子转移级联过程偶联亚氨基醚和烯醇重氮乙酸酯。包括恶唑啉、苯并恶唑和苯甲亚胺酯在内的一般亚氨基醚类是这些反应的适用底物，可直接获得具有均匀高化学和区域选择性的完全取代的吡咯。吡咯 2-、5- 和 N-位取代的高度可变性表征了这种方法，该方法也提供了通过对所得 N-官能吡咯的轻松修饰来进一步实现吡咯多样化的切入点。

  DOI：

  10.1002/anie.202101641
• 作为产物：
  描述：

  2-叠氮基乙醇 、 特戊醛 在 三氟化硼乙醚 作用下， 以 二氯甲烷 为溶剂， 反应 2.0h， 以76%的产率得到2-tert-butyl-oxazoline
  参考文献：
  名称：

  One-Step Conversion of Aldehydes to Oxazolines and 5,6-Dihydro-4H-1,3-oxazines Using 1,2- and 1,3-Azido Alcohols

  摘要：

  The reactions of 1,2- and 1,3-hydroxy azides with aldehydes under acidic conditions were examined. A variety of Lewis acids were examined, of which BF3 . OEt(2) was found the most convenient. Trimethylsilyl ether derivatives of the alcohols could also be reacted using trimethylsilyl triflate as the promoter. Twenty-five examples that proceed in moderate to quantitative yields are reported.

  DOI：

  10.1021/jo9521256

文献信息

• CYCLOALKENYL ARYL DERIVATIVES FOR CETP INHIBITOR
  申请人：Lee SeoHee

  公开号：US20140031335A1

  公开（公告）日：2014-01-30

  The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same. The compounds of the present invention show the effect of CETP activity inhibition. It means that the compounds can increase HDL-cholesterol and decrease LDL-cholesterol.

  本发明涉及环烯基芳基衍生物及其异构体、药学上可接受的盐、水合物或溶剂合物；制备这些衍生物的方法；以及含有这些衍生物的药物组合物。本发明的化合物显示出CETP活性抑制的效果。这意味着这些化合物可以增加HDL-胆固醇并降低LDL-胆固醇。
• COMPOUNDS USEFUL AS INHIBITORS OF PROTEIN KINASES
  申请人：Vasudevan Anil

  公开号：US20100035919A1

  公开（公告）日：2010-02-11

  Disclosed herein are compounds of formula (I) or pharmaceutical acceptable salts thereof, wherein A, X 1 , X 2 , R 1 , R 2 , R 3 , m, n, and p are defined in the specification. Compositions including the compounds which can be useful for inhibiting Rho kinase (ROCK) and methods for using the compositions are also described.

  本文披露了式（I）的化合物或其药用可接受的盐，其中A、X1、X2、R1、R2、R3、m、n和p在规范中有定义。还描述了包括这些化合物的组合物，这些组合物可用于抑制Rho激酶（ROCK），并描述了使用这些组合物的方法。
• BENZODIAZEPINE DERIVATIVES, COMPOSITIONS, AND METHODS FOR TREATING COGNITIVE IMPAIRMENT
  申请人：AgeneBio, Inc.

  公开号：US20180170941A1

  公开（公告）日：2018-06-21

  This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those benzodiazepine derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of a α5-containing GABA A receptor agonist (e.g., a α5-containing GABA A receptor positive allosteric modulator) as described herein in treating cognitive impairment associated with central nervous system (CNS) disorders in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI (aMCI), Age-Associated Memory Impairment (AAMI), Age Related Cognitive Decline (ARCD), dementia, Alzheimer's Disease(AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease (PD), autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction. It also relates to the use of a α5-containing GABA A receptor agonist (e.g., a α5-containing GABA A receptor positive allosteric modulator) as described herein in treating brain cancers (including brain tumors, e.g., medulloblastomas), and cognitive impairment associated therewith.

  这项发明涉及苯二氮卓啉衍生物，包括含有这些苯二氮卓啉衍生物的治疗有效量的组合物，以及使用这些衍生物或组合物治疗与中枢神经系统（CNS）疾病相关的认知障碍的方法。具体而言，它涉及在需要或有风险的受试者中治疗与中枢神经系统（CNS）疾病相关的认知障碍，包括但不限于患有或有风险患有与年龄相关的认知障碍、轻度认知障碍（MCI）、遗忘性MCI（aMCI）、年龄相关记忆障碍（AAMI）、年龄相关认知衰退（ARCD）、痴呆症、阿尔茨海默病（AD）、前驱期AD、创伤后应激障碍（PTSD）、精神分裂症、躁郁症、肌萎缩侧索硬化（ALS）、癌症治疗相关认知障碍、智力障碍、帕金森病（PD）、自闭症谱系障碍、脆性X综合症、瑞特综合症、强迫行为和物质成瘾。它还涉及在治疗与之相关的脑癌（包括脑肿瘤，例如髓母细胞瘤）和认知障碍的情况下，如本文所述使用α5含有的GABAA受体激动剂（例如，α5含有的GABAA受体正向变构调节剂）。
• Novel benzylamine derivatives and their utility as cholesterol ester-transfer protein inhibitors
  申请人：Baruah Anima

  公开号：US20070015758A1

  公开（公告）日：2007-01-18

  The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.

  本发明提供了新的苄基胺化合物，包括苄基胺化合物的组合物，制备苄基胺化合物的方法，以及使用苄基胺化合物治疗或预防与脂蛋白代谢有关的各种疾病或症状的方法。
• Pyrrolo[2,1-F] [1,2,4] Triazin-4-Ylamines IGF-1R Kinase Inhibitors for the Treatment of Cancer and Other Hyperproliferative Diseases
  申请人：O'Connor Stephen

  公开号：US20110294776A1

  公开（公告）日：2011-12-01

  This invention relates to novel compounds of formula (I). Formula (I) in which the variable groups are as defined in the specification and claims, to pharmaceutical compositions containing them, and to a method of treatment using them for treatment of cancer.

  本发明涉及公式（I）的新化合物。公式（I）中变量基团如规范和要求中所定义，以及含有它们的制药组合物和使用它们治疗癌症的治疗方法。