(+)-methyl (2S,3R)-3-amino-2-methyl-3-phenylpropionate

• 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
• 英文名称: (+)-methyl (2S,3R)-3-amino-2-methyl-3-phenylpropionate
• 英文别名: methyl (2S,3R)-3-amino-2-methyl-3-phenylpropionate；methyl (2S,3R)-3-amino-2-methyl-3-phenylpropanoate
• 化学式: C₁₁H₁₅NO₂
• 分子量: 193.246
• InChiKey: KVMIEZCRDGCHLN-WCBMZHEXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  14
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  52.3
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (+)-methyl (2S,3R)-3-amino-2-methyl-3-phenylpropionate 在 ammonium hydroxide 作用下， 以 methanolic ammonia 为溶剂， 生成 (2S,3R)-3-amino-2-methyl-3-phenylpropionamide
  参考文献：
  名称：

  Substituted pyridine and pyridazine compounds and methods of use

  摘要：

  选定的小说替代吡啶和吡啶二氮化合物对于预防和治疗疾病，如TNF-α、IL-1β、IL-6和/或IL-8介导的疾病，以及其他疾病，如癌症、疼痛和糖尿病，具有有效性。该发明涵盖了新颖化合物、类似物、前药和其药学上可接受的盐，药物组合物以及用于预防和治疗涉及炎症、癌症、疼痛、糖尿病等疾病和其他疾病或病情的方法。该发明还涉及制备这类化合物的方法以及在这类方法中有用的中间体。

  公开号：

  US06174901B1
• 作为产物：
  描述：

  tert-butyl anti-2-(methoxycarbonyl)-1-phenylpropylcarbamate 以 四氢呋喃 、 二氯甲烷 为溶剂， 反应 1.0h， 以100%的产率得到(+)-methyl (2S,3R)-3-amino-2-methyl-3-phenylpropionate
  参考文献：
  名称：

  Lewis碱辅助的Bronsted碱催化：二齿膦氧化物作为Bronsted碱性镧-芳基氧化物的活化剂和调节剂。

  摘要：

  DOI：

  10.1002/anie.200803682

文献信息

• Substituted pyrimidinone and pyridone compounds and methods of use
  申请人：Amgen Inc.

  公开号：US06096753A1

  公开（公告）日：2000-08-01

  Selected novel substituted pyrimidinone and pyridone compounds are effective for prophylaxis and treatment of diseases, such as TNF-.alpha., IL-1.beta., IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

  所选的新型嘧啶酮和吡啶酮化合物对预防和治疗疾病（如TNF-alpha、IL-1beta、IL-6和/或IL-8介导的疾病）以及其他疾病（如疼痛和糖尿病）具有有效性。该发明涵盖了新型化合物、类似物、前药和其药学上可接受的盐，以及用于预防和治疗涉及炎症、疼痛、糖尿病等疾病和其他疾患或情况的药物组合物和方法。该发明还涉及制备这类化合物的方法，以及在这类方法中有用的中间体。
• Substituted pyridine and pyridazine compounds and methods of use
  申请人：Amgen Inc.

  公开号：US06174901B1

  公开（公告）日：2001-01-16

  Selected novel substituted pyridine and pyridazine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

  选定的小说替代吡啶和吡啶二氮化合物对于预防和治疗疾病，如TNF-α、IL-1β、IL-6和/或IL-8介导的疾病，以及其他疾病，如癌症、疼痛和糖尿病，具有有效性。该发明涵盖了新颖化合物、类似物、前药和其药学上可接受的盐，药物组合物以及用于预防和治疗涉及炎症、癌症、疼痛、糖尿病等疾病和其他疾病或病情的方法。该发明还涉及制备这类化合物的方法以及在这类方法中有用的中间体。
• Diastereoselective Synthesis of β-Amino Esters by the Lewis Acid-Mediated Reaction of<i>N</i>-Tosyl Aldimines with Ketene Bis(trimethylsilyl) Acetals
  作者：Shigeru Shimada、Kazuhiko Saigo、Masanori Abe、Atsushi Sudo、Masaki Hasegawa

  DOI：10.1246/cl.1992.1445

  日期：1992.8

  In the presence of titanium(IV) bromide, N-tosyl aldimines smoothly reacted with ketene bis(trimethylsilyl) acetals at low temperature, and upon esterification anti-β-amino esters were obtained selectively.

  在溴化钛 (IV) 存在下，N-甲苯磺酰醛亚胺在低温下与乙烯酮双（三甲基甲硅烷基）缩醛顺利反应，并通过酯化选择性地获得抗β-氨基酯。
• Substituted pyridone compounds and methods of use
  申请人：Amgen Inc.

  公开号：US20030073704A1

  公开（公告）日：2003-04-17

  Selected novel substituted pyrimidinone and pyridone compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

  选定的新型嘧啶酮和吡啶酮化合物对于预防和治疗疾病（如TNF-α、IL-1β、IL-6和/或IL-8介导的疾病）以及其他疾病（如疼痛和糖尿病）是有效的。该发明涵盖了新型化合物、类似物、前药和其药学上可接受的盐、制药组合物以及用于预防和治疗涉及炎症、疼痛、糖尿病等疾病和其他疾患或病况的方法。该发明还涉及制造这些化合物的过程以及在这些过程中有用的中间体。
• Substituted pyrimidine compounds and methods of use
  申请人：Amgen Inc.

  公开号：US06410729B1

  公开（公告）日：2002-06-25

  Selected novel substituted pyrimidine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

  选择的新型替代嘧啶化合物对于预防和治疗疾病非常有效，比如TNF-α、IL-1β、IL-6和/或IL-8介导的疾病，以及其他疾病，比如疼痛和糖尿病。该发明涵盖了新型化合物、类似物、前药和其药学上可接受的盐、药物组合物和预防和治疗涉及炎症、疼痛、糖尿病等疾病和其他疾病或病况的方法。该发明还涉及制备这些化合物的方法以及在这些过程中有用的中间体。