2-fluorobenzyl N-succinimidyl carbonate | 128595-02-8

• 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: 2-fluorobenzyl N-succinimidyl carbonate
• 英文别名: 1-({[(2-fluorobenzyl)oxy]carbonyl}oxy)pyrrolidine-2,5-dione；carbonic acid 2,5-dioxopyrrolidin-1-yl ester 2-fluorobenzyl ester；(2,5-Dioxopyrrolidin-1-yl) (2-fluorophenyl)methyl carbonate
• CAS: 128595-02-8
• 化学式: C₁₂H₁₀FNO₅
• 分子量: 267.214
• InChiKey: BBWHKHLMEUAKNR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  19
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  72.9
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  2-fluorobenzyl N-succinimidyl carbonate 、 H-Lys(Boc)-D-gGlu-Oic-OH 生成 (2S,3aS,7aS)-1-[(4R)-4-[[(2S)-6-amino-2-[(2-fluorophenyl)methoxycarbonylamino]hexanoyl]amino]-4-carboxybutanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carboxylic acid
  参考文献：
  名称：

  SAWAYAMA, TADAHIRO;TSUKAMOTO, MASATOSHI;SASAGAWA, TAKASHI;NISHIMURA, KAZU+, CHEM. AND PHARM. BULL., 38,(1990) N, C. 110-115

  摘要：

  DOI：
• 作为产物：
  描述：

  N,N'-二琥珀酰亚胺基碳酸酯 、 2-氟苄醇 在 4-二甲氨基吡啶 作用下， 以 二氯甲烷 、 乙腈 为溶剂， 反应 6.0h， 以58%的产率得到2-fluorobenzyl N-succinimidyl carbonate
  参考文献：
  名称：

  血管紧张素转化酶抑制剂：N-取代的三肽抑制剂的合成和生物学活性。

  摘要：

  合成了一系列新的高效血管紧张素转化酶（ACE）抑制剂，即1-（N2-取代的L-赖氨酰基-γ-D-谷氨酰基）八氢-1H-吲哚-2-羧酸。在N末端P1 Lys的α-氨基处引入了各种酰基。研究了N2-酰基对体外抑制活性和口服降压作用的影响。发现所有合成的N-酰基三肽都具有约纳摩尔水平的体外抑制活性，并且当口服时，在肾性高血压大鼠中以10 mg / kg的剂量显示出抗高血压功效。其中，化合物7e，g和9f，i，m与依那普利（2a）相比显示出有效且持久的降压作用。还讨论了它们的构效关系。

  DOI：

  10.1248/cpb.38.110

文献信息

• [EN] 1-PHENYL-SUBSTITUTED HETEROCYCLYL DERIVATIVES AND THEIR USE AS PROSTAGLANDIN D2 RECEPTOR MODULATORS<br/>[FR] DÉRIVÉS D'HÉTÉROCYCLYLE SUBSTITUÉS PAR UN 1-PHÉNYLE ET LEUR UTILISATION EN TANT QUE MODULATEURS DES RÉCEPTEURS DE LA PROSTAGLANDINE D2
  申请人：ACTELION PHARMACEUTICALS LTD

  公开号：WO2012004722A1

  公开（公告）日：2012-01-12

  302 Abstract The present invention relates to 1-phenyl-substituted heterocyclyl derivatives of the formula (I), O Y R 5 R 6 N R 2 R 3 R 4 X Z R 1 R 7 R 7 R 10 n (I) 5 wherein X, Y, Z, n, R 1, R 2, R 3, R 4, R 5, R 6, R 7 and R 10 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D 2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation. 10

  本发明涉及公式(I)的1-苯基取代的杂环基衍生物，其中X、Y、Z、n、R1、R2、R3、R4、R5、R6、R7和R10如描述中所述，并且它们作为前列腺素受体调节剂的用途，特别是作为前列腺素D2受体调节剂，在治疗各种前列腺素介导的疾病和紊乱中的用途，以及含有这些化合物的制药组合物和其制备方法。
• [EN] 2-PYRIDYL AND 2-PYRIMIDYL CYCLOALKYLENE AMIDE COMPOUNDS AS NR2B RECEPTOR ANTAGONISTS<br/>[FR] 2-PYRIDYL-CYCLOALKYLENE-AMIDES ET 2-PYRIMIDYL-CYCLOALKYLENE-AMIDES CONSTITUANT DES ANTAGONISTES DU RECEPTEUR NR2B
  申请人：PFIZER JAPAN INC

  公开号：WO2004054579A1

  公开（公告）日：2004-07-01

  This invention provides a compound of the Formula (I), wherein R1 represents Formula (II), wherein R5 represents a hydroxy group or the like; R6 represents a hydrogen atom or the like. Z represents a carbon or a nitrogen atom: R2 represents a hydrogen atom or the like: R3 represents a hydrogen or the like: A represents a cycloalkylene or the like: X represents a covalent bond or the like: R4 represents an aryl or the like. These compounds are useful for the treatment of disease conditions caused by overactivation of NMDA NR2B receptor such as pain, or the like in mammals. This invention also provides a pharmaceutical composition comprising the above compound.

  本发明提供了一种Formula(I)化合物，其中R1代表Formula(II)，其中R5代表羟基或类似物；R6代表氢原子或类似物。Z代表一个碳原子或氮原子：R2代表氢原子或类似物：R3代表氢原子或类似物：A代表环烷基或类似物：X代表共价键或类似物：R4代表芳基或类似物。这些化合物对于治疗由NMDA NR2B受体过度激活引起的疾病状况如疼痛等在哺乳动物中是有用的。本发明还提供了包含上述化合物的制药组合物。
• Cycloalkylene amide compounds as NR2B receptor antagonists
  申请人：——

  公开号：US20040152715A1

  公开（公告）日：2004-08-05

  This invention provides a compound of the formula (I): 1 wherein R 1 represents 2 wherein R 5 represents a hydroxy group or the like; R 6 and R 7 independently represents a hydrogen atom or the like: V represents an alkylene or the like: W represents a carbon atom or the like: Z represents a carbon or the like: R 2 represents a hydrogen atom or the like: R 3 represents a hydrogen or the like: A represents a cycloalkylene or the like: X represents a covalent bond or the like: R 4 represents an aryl or the like. These compounds are useful for the treatment of disease conditions caused by overactivation of NMDA NR2B receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.

  本发明提供了式（I）的化合物： 1其中R1表示2其中R5表示羟基或类似物；R6和R7独立地表示氢原子或类似物：V表示烷基或类似物：W表示碳原子或类似物：Z表示碳或类似物：R2表示氢原子或类似物：R3表示氢或类似物：A表示环烷基或类似物：X表示共价键或类似物：R4表示芳基或类似物。这些化合物对于治疗由NMDA NR2B受体过度激活引起的疾病条件，如疼痛等哺乳动物疾病，非常有用。本发明还提供了包含上述化合物的制药组合物。
• 1-PHENYL-SUBSTITUTED HETEROCYCLYL DERIVATIVES AND THEIR USE AS PROSTAGLANDIN D2 RECEPTOR MODULATORS
  申请人：Aissaoui Hamed

  公开号：US20130109685A1

  公开（公告）日：2013-05-02

  The present invention relates to 1-phenyl-substituted heterocyclyl derivatives of the formula (I), wherein X, Y, Z, n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 10 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D 2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.

  本发明涉及公式（I）中1-苯基取代的杂环基衍生物，其中X、Y、Z、n、R1、R2、R3、R4、R5、R6、R7和R10如描述中所述，以及它们在各种前列腺素介导的疾病和疾病的治疗中作为前列腺素受体调节剂，特别是作为前列腺素D2受体调节剂的用途，以及包含这些化合物的制药组合物和它们的制备方法。
• Core-shell polymer particles
  申请人：The Goodyear Tire & Rubber Company

  公开号：US20040127603A1

  公开（公告）日：2004-07-01

  A core-shell particle for use as filler in rubber compositions. In one embodiment, the particle comprises a crosslinked core having repeat aromatic vinyl units. During an emulsion polymerization, a crosslinked shell comprising of conjugated diene units is grafted onto the core through residual vinyl units. The polymeric shell provides for better interaction and dispersion of the styrene core in an otherwise immiscible polymer matrix, particularly diene-based polymers. In another embodiment, the core has repeat units of (i) about 0% to about 25% by weight of a conjugated diene unit, (ii) about 70% to about 85% by weight of an aromatic vinyl unit, and (iii) about 15% to about 30% by weight of a crosslinking monomer unit.

  一种芯壳粒子，可用作橡胶组合物中的填料。在一个实施方案中，颗粒包括一个具有重复芳香族乙烯基单元的交联芯。在乳液聚合过程中，由共轭二烯单元组成的交联壳通过残余乙烯基单元接枝到芯上。这种聚合物外壳可使苯乙烯芯材在原本不相溶的聚合物基体（尤其是二烯基聚合物）中更好地相互作用和分散。在另一个实施方案中，芯材具有以下重复单元：(i) 约 0% 至约 25% （按重量计）共轭二烯单元；(ii) 约 70% 至约 85% （按重量计）芳香乙烯基单元；(iii) 约 15% 至约 30% （按重量计）交联单体单元。