2-bromophenyl phosphate | 134218-85-2

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 有机磷酸及其衍生物
• 英文名称: 2-bromophenyl phosphate
• 英文别名: phosphoric acid mono-(2-bromo-phenyl ester)；Phosphorsaeure-mono-(2-brom-phenylester)；(2-Brom-phenyl)-dihydrogenphosphat；Phenol, 2-bromo-, dihydrogen phosphate；(2-bromophenyl) dihydrogen phosphate
• CAS: 134218-85-2
• 化学式: C₆H₆BrO₄P
• 分子量: 252.989
• InChiKey: BXRXEOQDLYSFCZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  66.8
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-bromophenyl phosphate 在 吡啶 、 碘 作用下， 反应 3.0h， 生成
  参考文献：
  名称：

  Noort, D.; Marel, G. A. van der; Gen, A. van der, Recueil des Travaux Chimiques des Pays-Bas, 1991, vol. 110, # 2, p. 53 - 56

  摘要：

  DOI：
• 作为产物：
  描述：

  2-溴苯酚 在 三氯化铝 、 水 、 三氯氧磷 作用下， 反应 8.0h， 生成 2-bromophenyl phosphate
  参考文献：
  名称：

  Noort, D.; Marel, G. A. van der; Gen, A. van der, Recueil des Travaux Chimiques des Pays-Bas, 1991, vol. 110, # 2, p. 53 - 56

  摘要：

  DOI：

文献信息

• Aryl phosphate derivatives of d4T having activity against resistant HIV strains
  申请人：——

  公开号：US20040087549A1

  公开（公告）日：2004-05-06

  Methods of inhibiting virus replication of in a cell infected with a resistant strain of HIV that includes administering to the infected cell a virus replication inhibiting amount of an aryl phosphate derivative of d4T.

  抑制HIV耐药株感染细胞中病毒复制的方法包括向感染细胞内施加一定量的d4T的芳基磷酸酯衍生物，以抑制病毒复制。
• [EN] ARYL PHOSPHATE DERIVATIVES OF d4T HAVING ANTI-HIV ACTIVITY<br/>[FR] DERIVES DE PHOSPHATE ARYLIQUE DE D4T POSSEDANT UNE ACTIVITE ANTI-VIH
  申请人：WAYNE HUGHES INST

  公开号：WO2000000501A1

  公开（公告）日：2000-01-06

  Aryl phosphate nucleosise derivatives of formula (I) show potent activity against HIV without undesirable levels of cytotoxic activity. Examples of aryl phosphate nucleoside derivatives include aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. In a preferred aspect of the present invention, the phosphorus of the aryl phosphate group is further substituted with an amino acid residue that may be esterified or substituted, such as a methoxy alaninyl group. In said formula, Y is oxygen or sulfur; R1 is unsubstituted aryl or aryl substituted with an electron-withdrawing group; R2 is a nucleoside of formula (II or III).

  化合物(I)的芳基磷酸核苷衍生物具有对HIV的强效活性，而不具有不良水平的细胞毒性。芳基磷酸核苷衍生物的例子包括d4T的芳基磷酸衍生物，其在芳基上带有对位溴代取代基。特别地，这些衍生物是HIV反转录酶的强效抑制剂。在本发明的首选方面中，芳基磷酸基的磷还进一步取代为氨基酸残基，该氨基酸残基可以被酯化或取代，例如甲氧基丙氨酰基团。在上述公式中，Y是氧或硫；R1是未取代的芳基或带有电子吸引基团的芳基；R2是公式(II或III)的核苷。
• [EN] PROCESS FOR MAKING FARNESYL-PROTEIN TRANSFERASE INHIBITORS<br/>[FR] PROCEDE DE PRODUCTION D'INHIBITEURS DE FARNESYL-PROTEINE TRANSFERASE
  申请人：MERCK & CO INC

  公开号：WO2000001691A1

  公开（公告）日：2000-01-13

  The present invention is directed to the improved synthesis of compounds of formula (I): which may be useful as farnesyl-protein transferase inhibitors. The present invention is also directed to the crystal forms of the monohydrate and mon-hydrochloride salt of 1-(3-Chlorophenyl)-4-[1-(4-cyanobenzyl)-5-imidazolylmethyl]-2-piperazinone.

  本发明旨在改进化合物(I)的合成，该化合物可用作法尼酰丙氨酸蛋白转移酶抑制剂。本发明还涉及1-(3-氯苯基)-4-[1-(4-氰基苯甲基)-5-咪唑甲基]-2-哌嗪酮的单水合物和单盐酸盐的晶体形式。
• Aryl phosphate derivatives of d4T having anti-HIV activity
  申请人：Parker Hughes Institute

  公开号：US20040171577A1

  公开（公告）日：2004-09-02

  Aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group show markedly increased potency as anti-HIV agents without undesirable levels of cytotoxic activity. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. In a preferred aspect of the present invention, the phosphorus of the aryl phosphate group is further substituted with an amino acid residue that may be esterified or substituted, such as a methoxy alaninyl group.

  苯基磷酸酯衍生物d4T的苯基上带有对位溴取代基，表现出明显增强的抗HIV活性，而不会产生不良的细胞毒性。特别地，这些衍生物是HIV反转录酶的有效抑制剂。在本发明的首选方面，苯基磷酸酯基的磷还进一步取代了氨基酸残基，可以酯化或取代，例如甲氧基丙氨酰基。
• Aryl Phosphate Derivatives of d4T having Activity Against Resistant HIV Strains
  申请人：Uckun M. Fatih

  公开号：US20070015733A1

  公开（公告）日：2007-01-18

  Methods of inhibiting virus replication of in a cell infected with a resistant strain of HIV that includes administering to the infected cell a virus replication inhibiting amount of an aryl phosphate derivative of d4T.

  抑制耐药HIV感染细胞中病毒复制的方法包括向感染的细胞中投入一定量的d4T的芳基磷酸酯衍生物，以抑制病毒的复制。