N-甲酰甘氨酸叔丁酯 | 51354-15-5

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: N-甲酰甘氨酸叔丁酯
• 英文名称: N-formyl-tert-butyl glycinate
• 英文别名: tert-butyl 2-formamidoacetate；Glycine, N-formyl-, 1,1-dimethylethyl ester
• CAS: 51354-15-5
• 化学式: C₇H₁₃NO₃
• 分子量: 159.185
• InChiKey: AWCUWCRQTQPXLK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  11
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.71
• 拓扑面积：
  55.4
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-甲酰甘氨酸叔丁酯 在 三乙胺 、 三氯氧磷 作用下， 以 二氯甲烷 为溶剂， 反应 0.58h， 以87%的产率得到异氰基乙酸叔丁酯
  参考文献：
  名称：

  Enantioselective synthesis of (−)-chloramphenicol via silver-catalysed asymmetric isocyanoacetate aldol reaction

  摘要：

  报告了一种基于4-硝基苯甲醛和苄基异氰基醋酸之间的催化不对称醇醛反应的（-）-氯霉素的简洁合成方法。

  DOI：

  10.1039/c5ob02141c
• 作为产物：
  描述：

  氯乙酸叔丁酯 以 甲醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 4.0h， 生成 N-甲酰甘氨酸叔丁酯
  参考文献：
  名称：

  Meduna, V.; Sawlewicz, P.; Vogt, R., Synthetic Communications, 1989, vol. 19, # 9-10, p. 1487 - 1492

  摘要：

  DOI：

文献信息

• A Straightforward Approach towards Cyclic Photoactivatable Tubulysin Derivatives
  作者：Judith Hoffmann、Uli Kazmaier

  DOI：10.1002/anie.201405650

  日期：2014.10.13

  synthesis of cyclic photoactivatable natural products. Cyclization occurs between the allyl moiety in the protecting group and a second double bond in the target molecule by means of ring‐closing metathesis. Cyclization should increase the metabolic stability towards proteases. On the other hand, the conformational change should cause diminished biological activity. As illustrated for tubulysin derivatives

  含有另外的烯丙基官能团的新的对光不稳定的保护基的开发允许合成可光活化的环状天然产物。通过闭环复分解，保护基中的烯丙基部分与靶分子中的第二个双键之间发生环化。环化应增加对蛋白酶的代谢稳定性。另一方面，构象变化应导致生物活性降低。如针对微管蛋白溶素衍生物所示，从Ugi反应和闭环易位的简单构造单元中，只需两个步骤即可轻松获得环状和可光活化的候选药物。在Ugi反应过程中，通过异氰酸酯组分引入光不稳定的保护基。
• [EN] BENZODIAZEPINE DERIVATIVES, COMPOSITIONS, AND METHODS FOR TREATING COGNITIVE IMPAIRMENT<br/>[FR] DÉRIVÉS DE BENZODIAZÉPINE, COMPOSITIONS ET MÉTHODES DE TRAITEMENT DE LA DÉFICIENCE COGNITIVE
  申请人：MEKONNEN BELEW

  公开号：WO2016205739A1

  公开（公告）日：2016-12-22

  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 GABAA receptor agonist (e.g., a α5-containing GABAA 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.

  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，包括但不限于具有或有风险患上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、雷特综合症、强迫行为和物质成瘾。
• 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）。
• [EN] 4-PHENOXYMETHYLPIPERIDINES AS MODULATORS OF GPR119 ACTIVITY<br/>[FR] 4-PHÉNOXYMÉTHYLPIPÉRIDINES COMME MODULATEURS DE L'ACTIVITÉ DE GPR119
  申请人：IRM LLC

  公开号：WO2010006191A1

  公开（公告）日：2010-01-14

  The present invention provides compounds of Formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent; diseases or disorders associated with the activity of GPR119.

  本发明提供了一种具有I式化合物的药物组合物，以及使用这种化合物来治疗或预防与GPR119活性相关的疾病或紊乱的方法。
• PDK4 INHIBITOR AND USE THEREOF
  申请人：THE KITASATO INSTITUE

  公开号：US20150344404A1

  公开（公告）日：2015-12-03

  The present invention to provide a novel pyruvate dehydrogenase kinase inhibitors. A pyruvate dehydrogenase kinase inhibitor comprising a compound represented by the general formula (I) as an active ingredient (wherein, ring A represents a 6-membered aromatic hydrocarbon ring optionally substituted with 2-4 substituents, R 1 and R 4 , which are the same or different, represent a hydrogen atom, a hydroxyl group, an optionally substituted C1-6 alkyl group, R 2 and R 3 , which are the same or different, represent a hydrogen atom, a carboxyl group, an optionally substituted C1-6 alkyl group, an optionally substituted C6-10 aryl group, or a group represented by —C (═R 9 )—R 10 ), a pharmaceutical composition for treatment or prophylaxis of diseases or disorders that pyruvate dehydrogenase kinase relates to its development or aggravation, and a cosmetic composition, and the like.

  本发明提供了一种新型丙酮酸脱氢酶激酶抑制剂。一种丙酮酸脱氢酶激酶抑制剂包括一种以通式(I)表示的化合物作为活性成分（其中，环A代表一个6-成员芳香碳氢环，可选择地取代有2-4个取代基，R1和R4，它们相同或不同，代表氢原子，羟基，可选择地取代的C1-6烷基基团，R2和R3，它们相同或不同，代表氢原子，羧基，可选择地取代的C1-6烷基基团，可选择地取代的C6-10芳基基团，或由—C(═R9)—R10表示的基团），一种用于治疗或预防与丙酮酸脱氢酶激酶有关的疾病或紊乱的药物组合物，以及一种化妆品组合物等。