3-methoxy-N-methylpyridin-2-amine | 902837-10-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 3-methoxy-N-methylpyridin-2-amine
• CAS: 902837-10-9
• 化学式: C₇H₁₀N₂O
• mdl: MFCD08061117
• 分子量: 138.169
• InChiKey: GOMBDEGBFABWLJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.285
• 拓扑面积：
  34.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-methoxy-N-methylpyridin-2-amine 在 正丁基锂 、 间氯过氧苯甲酸 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 反应 2.0h， 生成 N-(3-methoxypyridin-2-yl)-N-methyl-P,P-diphenylphosphinic amide
  参考文献：
  名称：

  通过 Pd(II) 催化的对映选择性 C-H 炔基化合成 P-立体磷酰胺

  摘要：

  P-立体膦酰胺代表手性有机催化剂和生物活性化合物中的重要结构元素。在此，我们报道了使用廉价的市售L-焦谷氨酸作为手性配体，Pd(II) 催化的对映选择性 C-H 炔基化反应。通过去对称化和动力学拆分，以良好的收率和高对映选择性制备了一系列结构多样的P -立体膦酰胺。定制的拥挤导向基团N-乙基-N- (3-甲基吡啶-2-基)氨基对于反应活性至关重要。

  DOI：

  10.1021/acs.orglett.3c01865

文献信息

• Pyrimidine derivatives useful as inhibitors of PKC-theta
  申请人：Barbosa J.M. Antonio

  公开号：US20060025433A1

  公开（公告）日：2006-02-02

  Disclosed are novel compounds of formula (I): wherein X, Y, R 1 , R 2 and R 3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

  披露了公式(I)的新颖化合物：其中X、Y、R1、R2和R3如本文所述定义，它们作为PKC-theta的抑制剂是有用的，因此可用于治疗通过PKC-theta活性介导或维持的多种疾病和失调，包括免疫失调和II型糖尿病。本发明还涉及包含这些化合物的药物组合物、使用这些化合物治疗各种疾病和失调的方法、制备这些化合物的方法以及在这些过程中有用的中间体。
• [EN] 5-(3-AMINOPHENYL)-5-ALKYL-5,6-DIHYDRO-2H-[1,4]OXAZIN-3-AMINE DERIVATIVES<br/>[FR] DÉRIVÉS DE 5-(3-AMINOPHÉNYL)-5-ALKYL-5,6-DIHYDRO-2H-[1,4]OXAZIN-3-AMINE
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2013083556A1

  公开（公告）日：2013-06-13

  The present invention relates to novel 5-(3-aminophenyl)-5-alkyl-5,6-dihydro- 2H-[1,4]oxazin-3-amine derivatives as inhibitors of beta-secretase, also known as beta- site amyloid cleaving enzyme, BACE, BACE 1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, cerebral amyloid angiopathy, multi-infarct dementia, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease and dementia associated with beta-amyloid. (Formula I)

  本发明涉及一种新型的5-(3-氨基苯基)-5-烷基-5,6-二氢-2H-[1,4]噁嗪-3-胺衍生物，作为β-分泌酶抑制剂，也被称为β-位点淀粉样蛋白裂解酶、BACE、BACE 1、Asp2或memapsin2。该发明还涉及包含这些化合物的药物组合物，用于制备这些化合物和组合物的工艺，以及利用这些化合物和组合物预防和治疗涉及β-分泌酶的疾病，如阿尔茨海默病（AD）、轻度认知障碍、老年痴呆、带有Lewy小体的痴呆、脑淀粉样脉管病、多梗塞性痴呆、唐氏综合征、与中风相关的痴呆、与帕金森病相关的痴呆以及与β-淀粉样蛋白相关的痴呆等疾病的治疗和预防。（化学式I）
• 5-(3-AMINOPHENYL)-5-ALKYL-5,6-DIHYDRO-2H-[1,4]OXAZIN-3-AMINE DERIVATIVES
  申请人：Janssen Pharmaceutica NV

  公开号：US20140364428A1

  公开（公告）日：2014-12-11

  The present invention relates to novel 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2H-[1,4]oxazin-3-amine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, cerebral amyloid angiopathy, multi-infarct dementia, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease and dementia associated with beta-amyloid.

  本发明涉及一种新型5-(3-氨基苯基)-5-烷基-5,6-二氢-2H-[1,4]噁嗪-3-胺衍生物，作为β-分泌酶抑制剂，也被称为β-位点淀粉样蛋白裂解酶、BACE、BACE1、Asp2或memapsin2。该发明还涉及包含这些化合物的药物组合物，用于制备这些化合物和组合物的方法，以及将这些化合物和组合物用于预防和治疗涉及β-分泌酶的疾病，如阿尔茨海默病（AD）、轻度认知障碍、老年痴呆、带有Lewy小体的痴呆、脑淀粉样血管病、多发性梗塞性痴呆、唐氏综合征、中风相关的痴呆、帕金森病相关的痴呆和β-淀粉样蛋白相关的痴呆。
• PYRIMIDINE DERIVATIVES USEFUL AS INHIBITORS OF PKC-THETA
  申请人：BARBOSA Antonio J.M.

  公开号：US20080287410A1

  公开（公告）日：2008-11-20

  Disclosed are novel compounds of formula (I): wherein X, Y, R 1 , R 2 and R 3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

  本发明涉及一种新型化合物，其化学式为（I）：其中X，Y，R1，R2和R3的定义如本文所述，该化合物可用作PKC-theta的抑制剂，因此可用于治疗多种通过PKC-theta的活性介导或维持的疾病和疾病，包括免疫性疾病和2型糖尿病。本发明还涉及包含这些化合物的制药组合物，使用这些化合物治疗各种疾病和疾病的方法，制备这些化合物的过程以及在这些过程中有用的中间体。
• SUBSTITUTED IMIDAZO[4,5-b]PYRIDINES AS INHIBITORS OF GASTRIC ACID SECRETION
  申请人：Nycomed GmbH

  公开号：EP1824850A2

  公开（公告）日：2007-08-29