di-p-tolylphosphinic azide | 4129-18-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: di-p-tolylphosphinic azide
• 英文别名: Di-(4-methylphenyl)-phosphinsaeureazid；Bis-p-tolyl-phosphonyl-azid；Bis-<4-tolyl>-phosphinsaeure-azid；Phosphinic azide, bis(4-methylphenyl)-；1-[azido-(4-methylphenyl)phosphoryl]-4-methylbenzene
• CAS: 4129-18-4
• 化学式: C₁₄H₁₄N₃OP
• 分子量: 271.258
• InChiKey: HGSNPZMQZQJDEO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  31.4
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  di-p-tolylphosphinic azide 、 甲醇 以33%的产率得到
  参考文献：
  名称：

  HARGER, M. J. P.;WESTLAKE, S., TETRAHEDRON, 1982, 38, N 10, 1511-1515

  摘要：

  DOI：
• 作为产物：
  描述：

  bis(4-methylphenyl)phosphinic acid 在 氯化亚砜 、 sodium azide 作用下， 以 乙腈 为溶剂， 反应 18.0h， 生成 di-p-tolylphosphinic azide
  参考文献：
  名称：

  二芳基次膦叠氮化物：光化学反应，包括在甲醇中的重排

  摘要：

  DOI：

  10.1016/0040-4020(82)80240-8

文献信息

• Intermediates for the synthesis of benzimidazole derivatives and a process for the preparation thereof
  申请人：SANKYO COMPANY, LIMITED

  公开号：US20030008907A1

  公开（公告）日：2003-01-09

  This invention provides a process for the preparation of a benzimidazole derivative (I) or a pharmaceutically acceptable salt thereof, 1 wherein R 1 is C 1 -C 6 alkyl, C 1 -C 6 alkoxyl, etc., R 2 is C 1 -C 6 alkyl, and R 3 is hydrogen or a protecting group, which exhibits excellent hyopoglycemic action, said process comprising condensation of an amine derivative (III) with a carboxylic acid derivatives (II) to afford a compound (IV), followed by cyclization of compound (IV) in the presence of an acid.

  本发明提供了一种制备苯并咪唑衍生物(I)或其药学上可接受的盐的方法，其中R1为C1-C6烷基，C1-C6烷氧基等，R2为C1-C6烷基，R3为氢或保护基，具有出色的降血糖作用，该方法包括将胺衍生物(III)与羧酸衍生物(II)缩合得到化合物(IV)，然后在酸的存在下使化合物(IV)环化。
• METHOD FOR MANUFACTURING A 6-SUBSTITUTED 1-METHYL-1H-BENZIMIDAZOLE DERIVATIVE AND AN INTERMEDIATE OF SAID METHOD
  申请人：Ikeuchi Yutaka

  公开号：US20120238759A1

  公开（公告）日：2012-09-20

  A method for manufacturing a 6-substituted 1-methyl-1H-benzimidazole derivative represented by the formula (IV) wherein R 3 represents a hydrogen atom or a C 1 -C 4 alkyl group. A 4-substituted N 2 -methylbenzene-1,2-diamine derivative is prepared from a particular 5-substituted N-methyl-2-nitroaniline derivative, subsequently reacting the resulting compound with 4-[(2,4-dioxo-1,3-thiazolidin-5-yl)methyl]phenoxy}acetic acid or an acid chloride or a mixed acid anhydride thereof, and subsequently subjecting the resulting compound to intramolecular dehydration condensation. A compound of the formula (II) wherein R 1 represents a hydrogen atom, a C 1 -C 4 alkyl group, or a protective group for the nitrogen atom, and R 2 represents a hydrogen atom or a protective group for the nitrogen atom is prepared and used as an intermediate.

  一种制备6-取代的1-甲基-1H-苯并咪唑衍生物的方法，该衍生物的化学式为（IV），其中R3代表氢原子或C1-C4烷基。首先从特定的5-取代N-甲基-2-硝基苯胺衍生物制备4-取代N2-甲基苯1,2-二胺衍生物，然后将所得化合物与4-[(2,4-二氧杂环戊烷-1,3-二酮-5-基)甲基]苯氧基}乙酸或其酸氯或混合酸酐反应，最后将所得化合物进行分子内脱水缩合反应。化合物的化学式为（II），其中R1代表氢原子、C1-C4烷基或氮原子的保护基，R2代表氢原子或氮原子的保护基，该化合物作为中间体使用。
• UREA TYPE CINNAMIDE DERIVATIVE
  申请人：Kimura Teiji

  公开号：US20100105904A1

  公开（公告）日：2010-04-29

  Disclosed is a compound represented by the formula (I) below or a pharmacologically acceptable salt thereof. Also disclosed is a use of the compound or salt as a pharmaceutical product. (In the formula, Ar 1 represents an imidazolyl group which may be substituted with a C 1-6 alkyl group; Ar 2 represents a phenyl group which may be substituted with a C 1-6 alkoxy group; X 1 represents a single bond; R 1 and R 2 respectively represent a C 1-6 alkyl group or the like which may be substituted with a substituent such as a 5- to 14-membered aromatic heterocyclic group; and R 3 represents a hydrogen atom or the like.)

  本发明涉及一种由下式（I）表示的化合物或其药学上可接受的盐。本发明还涉及该化合物或盐作为制药产品的用途。（在公式中，Ar1代表可以被C1-6烷基取代的咪唑基；Ar2代表可以被C1-6烷氧基取代的苯基；X1代表单键；R1和R2分别代表C1-6烷基或类似物，可以被5-至14-成员芳香杂环基等取代基取代；而R3代表氢原子或类似物。）
• INTERMEDIATES FOR THE SYNTHESIS OF BENZIMIDAZOLE COMPOUNDS AND PROCESS FOR THE PREPARATION THEREOF
  申请人：Sankyo Company, Limited

  公开号：EP1191019A1

  公开（公告）日：2002-03-27

  This invention provides a process for the preparation of a benzimidazole derivative (I) or a pharmaceutically acceptable salt thereof, wherein R1 is C1-C6 alkyl, C1-C6 alkoxyl, etc., R2 is C1-C6 alkyl, and R3 is hydrogen or a protecting group, which exhibits excellent hyopoglycemic action, said process comprising condensation of an amine derivative (III) with a carboxylic acid derivatives (II) to afford a compound (IV), followed by cyclization of compound (IV) in the presence of an acid.

  本发明提供了一种苯并咪唑衍生物(I)或其药学上可接受的盐的制备方法、 其中，R1 为 C1-C6 烷基、C1-C6 烷氧基等，R2 为 C1-C6 烷基，R3 为氢或保护基团，具有优异的降血糖作用，所述工艺包括胺衍生物 (III) 与羧酸衍生物 (II) 缩合得到化合物 (IV)，然后化合物 (IV) 在酸存在下环化。
• Intermediates for the synthesis of benzimidazole compounds and process for the preparation thereof
  申请人：Sankyo Company Limited

  公开号：EP1607385A1

  公开（公告）日：2005-12-21

  This invention provides a process for the preparation of a benzimidazole derivative (9) or a pharmaceutically acceptable salt thereof, by condensation of a compound of formula (6) with a compound of formula (7) in the presence of a condensing agent to afford a compound of formula (8), followed by, if necessary removal of the amino protecting group of compound (8), and then cyclization of compound (8) in the presence of an acid, wherein R1e, R2e, R3e and R4e are each independently hydrogen, hydroxyl, alkyl, alkoxy, benzyloxy, acetoxy, trifluoromethyl or halogen, R7e is alkyl and R8e is hydrogen or an amino protecting group, wherein R1e, R2e, R3e, R4e, R7e and R8e are as defined above, wherein R1e, R2e, R3e, R4e, and R7e are as defined above.

  本发明提供了一种制备苯并咪唑衍生物（9）或其药学上可接受的盐的工艺，其方法是：在缩合剂存在下，将式（6）化合物与式（7）化合物缩合，得到式（8）化合物，然后必要时去除化合物（8）的氨基保护基，再在酸存在下将化合物（8）环化、 其中 R1e、R2e、R3e 和 R4e 各自独立地为氢、羟基、烷基、烷氧基、苄氧基、乙酰氧基、三氟甲基或卤素，R7e 为烷基，R8e 为氢或氨基保护基、 其中 R1e、R2e、R3e、R4e、R7e 和 R8e 如上定义、 其中 R1e、R2e、R3e、R4e 和 R7e 如上定义。