N-{[4-(3,4-Dichlorobenzyl)morpholin-2-yl]methyl}-2-(5-methyl-2-phenyl-1,3-oxazol4-yl)acetamide | 407637-86-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: N-{[4-(3,4-Dichlorobenzyl)morpholin-2-yl]methyl}-2-(5-methyl-2-phenyl-1,3-oxazol4-yl)acetamide
• 英文别名: N-{[4-(3,4-Dichlorobenzyl)morpholin-2-yl]methyl]-2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)acetamide；N-[[4-[(3,4-dichlorophenyl)methyl]morpholin-2-yl]methyl]-2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)acetamide
• CAS: 407637-86-9
• 化学式: C₂₄H₂₅Cl₂N₃O₃
• 分子量: 474.387
• InChiKey: FGUIUYGIZLOOHE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  32
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  67.6
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  [4-(3,4-dichlorobenzyl)morpholin-2-yl]methylamine 、 2-（5-甲基-2-苯基1，3-氧杂醇-4-烷基）乙酸 以to give the title compound (0.036 g)的产率得到N-{[4-(3,4-Dichlorobenzyl)morpholin-2-yl]methyl}-2-(5-methyl-2-phenyl-1,3-oxazol4-yl)acetamide
  参考文献：
  名称：

  Process for the preparation of morpholine derivatives and intermediates therefore

  摘要：

  本发明揭示了制备式（IIIA）化合物或其盐的过程。

  公开号：

  US20050222147A1

文献信息

• Morpholin-acetamide derivatives for the treatment of inflammatory diseases
  申请人：——

  公开号：US20040058923A1

  公开（公告）日：2004-03-25

  Compounds of formula (I) wherein: R 1 represents C 1-16 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 2-6 alkynyl-Y 1 —, aryl-Y 1 —, heteroaryl-Y 1 —, aryl-(O) t -aryl-Y 1 —, aryl-(O) t -heteroaryl-Y 1 —, heteroaryl-(O) t -aryl-Y 1 —, heteroaryl-(O) t -heteroaryl-Y 1 —, C 2-6 alkenyl-Y 1 —, aryl-O—Y 1 —, heteroaryl-O—Y 1 —, C 1-16 alkyl-SO 2 —Y 1 —,M—Y 1 —,J 2 -Y 1 —, —CN or C 3-8 cycloalkyl-Y 1 — or C 3-8 cycloalkenyl-Y 1 —, which cycloalkyl or cycloalkenyl may be optionally substituted by one or more hydroxyl or C 1-16 Alkyl groups; R 2 represents hydrogen or C 1-16 alkyl; X represents ethylene or a group of formula CR e R f wherein R e and R f independently represent hydrogen or C 1-14 alkyl or R e and R f may together with the carbon atom to which they are attached form a C 3-8 cycloalkyl group; R 3 and R 4 independently represent hydrogen or C 1-14 alkyl; Z represents a bond, CO, SO 2 , CR 9 R 6 (CH 2 ) n , (CH 2 ) n CR 9 R 6 , CHR 6 (CH 2 ) n O, CHR 6 (CH 2 ) n S, CHR 6 (CH 2 ) n OCO, CHR 6 (CH 2 ) n CO, COCHR 6 (CH 2 ) n or SO 2 CHR 6 (CH 2 ) n ; n represents an integer from 0 to 4; processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases. 1

  式(I)的化合物，其中：R1代表C1-16烷基，C2-6烯基，C2-6炔基，C2-6炔基-Y1—，芳基-Y1—，杂环芳基-Y1—，芳基-(O)t-芳基-Y1—，芳基-(O)t-杂环芳基-Y1—，杂环芳基-(O)t-芳基-Y1—，杂环芳基-(O)t-杂环芳基-Y1—，C2-6烯基-Y1—，芳基-O—Y1—，杂环芳基-O—Y1—，C1-16烷基-SO2—Y1—，M—Y1—，J2-Y1—，—CN或C3-8环烷基-Y1—或C3-8环烯基-Y1—，其中环烷基或环烯基可以选择地被一个或多个羟基或C1-16烷基基团取代；R2代表氢或C1-16烷基；X代表乙烯或公式CReRf的基团，其中Re和Rf独立地代表氢或C1-14烷基，或Re和Rf可以与它们连接的碳原子一起形成C3-8环烷基基团；R3和R4独立地代表氢或C1-14烷基；Z代表键，CO，SO2，CR9R6(CH2)n，( )nCR9R6，CHR6( )nO，CHR6( )nS，CHR6( )nOCO，CHR6( )nCO，COCHR6( )n或SO2CHR6( )n；n代表一个从0到4的整数；它们的制备方法，包含它们的配方以及它们在治疗炎症性疾病中的用途。
• MORPHOLIN-ACETAMIDE DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISEASES
  申请人：Ancliff Rachael Anne

  公开号：US20090163495A1

  公开（公告）日：2009-06-25

  There are provided according to the invention, novel compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , X, a, b and Z are as defined in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.

  根据本发明提供了新的化合物，化学式为（I），其中R1、R2、R3、R4、R5、X、a、b和Z的定义如规范中所述，制备它们的方法，包含它们的配方以及它们在治疗炎症性疾病中的应用。
• US7560548B2
  申请人：——

  公开号：US7560548B2

  公开（公告）日：2009-07-14
• [EN] MORPHOLIN-ACETAMIDE DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISEASES<br/>[FR] DERIVES DE MORPHOLINE-ACETAMIDE PERMETTANT DE TRAITER LES MALADIES INFLAMMATOIRES
  申请人：GLAXO GROUP LTD

  公开号：WO2002026722A1

  公开（公告）日：2002-04-04

  Compounds of formula (I) wherein: R1 represents C¿1-16? alkyl, C2-6alkenyl, C2-6alkynyl, C2-6alkynyl-Y?1¿-, aryl-Y1-, heteroaryl-Y1-, aryl-(O)¿t?-aryl-Y?1¿-, aryl-(O)¿t?-heteroaryl-Y?1¿-, heteroaryl-(O)¿t?-aryl-Y?1¿-, heteroaryl-(O)¿t?-heteroaryl-Y?1¿-, C¿2-6? alkenyl-Y?1¿-, aryl-O-Y1-, heteroaryl-O-Y1-, C¿1-16? alkyl-SO2-Y?1-,M-Y1-,J2-Y1¿-, -CN or C¿3-8? cycloalkyl-Y?1¿-or C¿3-8? cycloalkenyl-Y?1¿-, which cycloalkyl or cycloalkenyl may be optionally substituted by one or more hydroxyl or C¿1-16? Alkyl groups; R?2¿ represents hydrogen or C¿1-16? alkyl; X represents ethylene or a group of formula CR?eRf¿ wherein R?e and Rf¿ independently represent hydrogen or C1-14 alkyl or R?e and Rf¿ may together with the carbon atom to which they are attached form a C¿3-8? cycloalkyl group; R?3 and R4¿ independently represent hydrogen or C¿1-14? alkyl; Z represents a bond, CO, SO2, CR?9R6(CH¿2)n, (CH2)nCR?9R6, CHR6(CH¿2)nO, CHR6(CH2)nS, CHR6(CH2)nOCO, CHR6(CH2)nCO, COCHR6(CH2)n or SO2CHR6(CH2)n; n represents an integer from 0 to 4; processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.