3-Carboxypropylidenetriphenylphosphorane | 63129-91-9

• 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: 3-Carboxypropylidenetriphenylphosphorane
• 英文别名: 3-(Triphenyl-lambda5-phosphanylidene)propanoic acid；3-(triphenyl-λ5-phosphanylidene)propanoic acid
• CAS: 63129-91-9
• 化学式: C₂₁H₁₉O₂P
• 分子量: 334.354
• InChiKey: QAVFOJFLRPJOLV-UHFFFAOYSA-N

物化性质

• 沸点：
  537.3±52.0 °C(Predicted)
• 密度：
  1.21±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  24
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  37.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  3-Carboxypropylidenetriphenylphosphorane 、 2-oxa-6-syn-<3αβ-(tetrahydropyran-2-yloxy)-4-phenoxy-1-trans-butenyl>-7-anti-(tetrahydropyran-2-yloxy)-cis-bicyclo<3.3.0>octan-3-ol 以 二甲基亚砜 为溶剂， 反应 2.0h， 生成 (Z)-5-[(1R,2R,3R,5S)-5-Hydroxy-2-[(E)-4-phenoxy-3-(tetrahydro-pyran-2-yloxy)-but-1-enyl]-3-(tetrahydro-pyran-2-yloxy)-cyclopentyl]-pent-3-enoic acid
  参考文献：
  名称：

  Prostaglandin analogs possessing antinidatory effects. 2. Modification of the .alpha. chain

  摘要：

  Additional double bonds were introduced into the alpha chain in 16-phenoxy-, 16-(3-chlorophenoxy)-, 16-[3-(tri-fluoromethyl)phenoxy]-, and 16-(4-chlorophenoxy)-17,18,19,20-tetranorprostaglandins which have antinidatory effects. Of these analogues, the delta 3-cis-delta 5 analogues 23b is 1200 times more potent than prostaglandin F2 alpha in antinidatory effect in the rat and more potent than any other known prostaglandin analogues.

  DOI：

  10.1021/jm00179a011
• 作为产物：
  描述：

  2-羧乙基三苯基溴化磷 在 sodiomethylsulfinyl carbaniom 作用下， 以 二甲基亚砜 为溶剂， 生成 3-Carboxypropylidenetriphenylphosphorane
  参考文献：
  名称：

  Prostaglandin analogs possessing antinidatory effects. 2. Modification of the .alpha. chain

  摘要：

  Additional double bonds were introduced into the alpha chain in 16-phenoxy-, 16-(3-chlorophenoxy)-, 16-[3-(tri-fluoromethyl)phenoxy]-, and 16-(4-chlorophenoxy)-17,18,19,20-tetranorprostaglandins which have antinidatory effects. Of these analogues, the delta 3-cis-delta 5 analogues 23b is 1200 times more potent than prostaglandin F2 alpha in antinidatory effect in the rat and more potent than any other known prostaglandin analogues.

  DOI：

  10.1021/jm00179a011

文献信息

• [EN] TUBULYSIN DERIVATIVES<br/>[FR] DÉRIVÉS DE TUBULYSINE
  申请人：MEDIMMUNE LLC

  公开号：WO2015157594A1

  公开（公告）日：2015-10-15

  Novel tubulysin derivatives which may be useful as cytotoxic agents to provide therapeutic benefits in the treatment of various types of cancers, alone or as drug conjugates with antibodies are provided. The tubulysin derivatives consist of a tetrapeptide scaffold comprising methyl and ethyl substituted piperidines. The tubulysin conjugates further comprise monoclonal antibody via succinimide linkers.

  提供了可能作为细胞毒性药物在治疗各种类型癌症中提供治疗益处的新型管肽衍生物，可以单独使用，也可以与抗体结合物作为药物共轭物。这些管肽衍生物由包含甲基和乙基取代哌啶的四肽支架组成。这些管肽结合物进一步包括通过琥珀酰亚胺连接剂连接的单克隆抗体。
• TUBULYSIN DERIVATIVES
  申请人：MedImmune LLC

  公开号：US20150291657A1

  公开（公告）日：2015-10-15

  Novel tubulysin derivatives which may be useful as cytotoxic agents to provide therapeutic benefits in the treatment of various types of cancers, alone, as drug conjugates or in combination with other chemotherapies are provided.

  提供了新型的管芸硫素衍生物，可用作细胞毒剂，在治疗各种癌症方面提供治疗效益，可以单独使用，作为药物结合物或与其他化疗药物联合使用。
• Hetera-aliphatic carboxamides
  申请人：ICI AMERICAS INC.

  公开号：EP0337766A1

  公开（公告）日：1989-10-18

  This invention provides a series of novel hetera-aliphatic carboxamides of formula I in which the group >Z-Y-X< is selected from >C=CH-N<, >N-CH=C<, >C=N-N< and >N-N=C< and the other radicals have the meanings defined in the following specification. The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically accept­able salts of the formula I compounds; pharmaceutical compositions containing the formula I compound, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.

  本发明提供了一系列式 I 的新型杂脂肪族羧酰胺，其中基团 >Z-Y-XC=CH-NN-CH=CC=N-NN-N=C<和其他基团具有以下说明书中定义的含义。式 I 的化合物是白三烯拮抗剂。本发明还提供了式 I 化合物的药学上可接受的盐；含有式 I 化合物或其盐的药物组合物，用于治疗例如过敏性或炎症性疾病，或内毒素性或创伤性休克病症；以及式 I 化合物的制造工艺和用于此类制造的中间体。
• Tocotrienols in the treatment of hypercholesterolemia, hyperlipidemia and thromboembolic disorders
  申请人：Bristol-Myers Squibb Company

  公开号：EP0421419A2

  公开（公告）日：1991-04-10

  This invention relates to the use of tocotrienol, gamma-tocotrienol and delta-tocotrienol in reducing hypercholesterolemia, hyperlipidemia and thromboembolic disorders in mammals. The isolation of these tocotrienols from natural sources and their chemical synthesis is disclosed. The present invention also relates to prodrugs and pharmaceutical compositions of gamma-tocotrienol, delta-tocotrienol and tocotrienol and uses thereof.

  本发明涉及生育三烯酚、γ-生育三烯酚和δ-生育三烯酚在降低哺乳动物高胆固醇血症、高脂血症和血栓栓塞性疾病方面的用途。本发明公开了从天然来源中分离这些生育三烯酚及其化学合成的方法。本发明还涉及γ-生育三烯酚、δ-生育三烯酚和生育三烯酚的原药和药物组合物及其用途。
• Tubulysin derivatives
  申请人：MedImmune LLC

  公开号：US10159745B2

  公开（公告）日：2018-12-25

  Novel tubulysin derivatives which may be useful as cytotoxic agents to provide therapeutic benefits in the treatment of various types of cancers, alone, as drug conjugates or in combination with other chemotherapies are provided.

  本研究提供了可用作细胞毒剂，在治疗各种类型癌症时单独使用、作为药物共轭物使用或与其他化疗药物联合使用时提供治疗效果的新型管胞素衍生物。