4-ethoxytriphenylmethanol | 62345-22-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 英文名称: 4-ethoxytriphenylmethanol
• 英文别名: (4-ethoxy-phenyl)-diphenyl-methanol；(4-Aethoxy-phenyl)-diphenyl-methanol；(4-Ethoxyphenyl)-diphenylmethanol
• CAS: 62345-22-6
• 化学式: C₂₁H₂₀O₂
• 分子量: 304.389
• InChiKey: WXRXJRIPBHXDLC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  23
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  29.5
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-ethoxytriphenylmethanol 在 氢溴酸 作用下， 以 苯 为溶剂， 反应 2.08h， 生成 4-ethoxytriphenylmethyl-O,O-diethylphosphonate
  参考文献：
  名称：

  Kopel'tsiv, Yu. A.; Kolesnikov, V. T.; Shermolovich, Yu. G., Journal of general chemistry of the USSR, 1986, vol. 56, # 3, p. 520 - 523

  摘要：

  DOI：
• 作为产物：
  描述：

  二苯甲酮 、 4-溴苯乙醚 在 正丁基锂 作用下， 以 四氢呋喃 、 正己烷 为溶剂， 反应 23.5h， 以64%的产率得到4-ethoxytriphenylmethanol
  参考文献：
  名称：

  Optimized S-Trityl-l-cysteine-Based Inhibitors of Kinesin Spindle Protein with Potent in Vivo Antitumor Activity in Lung Cancer Xenograft Models

  摘要：

  The mitotic kinesin Eg5 is critical for the assembly of the mitotic spindle and is a promising chemotherapy target. Previously, we identified S-trityl-L-cysteine as a selective inhibitor of Eg5 and developed triphenylbutanamine analogues with improved potency, favorable drug-like properties, but moderate in vivo activity. We report here their further optimization to produce extremely potent inhibitors of Eg5 (K-i(app) < 10 nM) with broad-spectrum activity against cancer cell lines comparable to the Phase II drug candidates ispinesib and SB-743921. They have good oral bioavailability and pharmacolcinetics and induced complete tumor regression in nude mice explanted with lung cancer patient xenografts. Furthermore, they display fewer liabilities with CYP-metabolizing enzymes and hERG compared with ispinesib and SB-743921, which is important given the likely application of Eg5 inhibitors in combination therapies. We present the case for this preclinical series to be investigated in single and combination chemotherapies, especially targeting hematological malignancies.

  DOI：

  10.1021/jm3014597

文献信息

• Amino acid loaded trityl alcohol resins, method of production of amino acid loaded trityl alcohol resins and therapeutics produced therewith
  申请人：Rohm and Haas Company

  公开号：EP1447408A1

  公开（公告）日：2004-08-18

  The present invention relates to a process for making a biologically active substance or therapeutic agent free of a chlorotrityl chloride linker-resin. The process includes reacting an activated amino acid or activated amino acid derivative with a substituted or unsubstituted trityl alcohol resin to obtain a resin-CT-AA product; and, reacting the resin-CT-AA product with other building blocks of the biologically active substance or therapeutic agent to obtain said biologically active substance or therapeutic. A product created by this process is also provided herein. The invention is particularly useful to create T-20 and T-1249 therapeutics.

  本发明涉及一种制造不含氯化三苯酯连接体-树脂的生物活性物质或治疗剂的工艺。该工艺包括使活化氨基酸或活化氨基酸衍生物与取代或未取代的三苯甲醇树脂反应，得到树脂-CT-AA 产物；以及使树脂-CT-AA 产物与生物活性物质或治疗剂的其他结构单元反应，得到所述生物活性物质或治疗剂。本发明还提供了通过该工艺制作的产品。本发明尤其适用于制造 T-20 和 T-1249 治疗剂。
• 852. Free radicals and radical stability. Part XIV. (Ethoxyphenyl)diphenylmethanols and the free radical (o-ethoxyphenyl)-diphenylmethyl
  作者：S. T. Bowden、D. T. Zalichi

  DOI：10.1039/jr9570004240

  日期：——
• KOPELTSIV, YU. A.;KOLESNIKOV, V. T.;SHERMOLOVICH, YU. G.;TROTSENKO, S. I.+, ZH. OBSHCH. XIMII, 1986, 56, N 3, 588-592
  作者：KOPELTSIV, YU. A.、KOLESNIKOV, V. T.、SHERMOLOVICH, YU. G.、TROTSENKO, S. I.+

  DOI：——

  日期：——
• PROCESS FOR PREPARING HIGH-REACTIVITY ISOBUTENE HOMO- OR COPOLYMERS
  申请人：BASF SE

  公开号：EP3416991A1

  公开（公告）日：2018-12-26
• Amino acid loaded trityl alcohol resins, method of production of amino acid loaded trityl alcohol resins and biologically active substances and therapeutics produced therewith
  申请人：——

  公开号：US20040158037A1

  公开（公告）日：2004-08-12

  The present invention relates to a process for making a biologically active substance or therapeutic agent free of a chlorotrityl chloride linker-resin. The process includes reacting an activated amino acid or activated amino acid derivative with a substituted or unsubstituted trityl alcohol resin to obtain a resin-CT-AA product; and, reacting the resin-CT-AA product with other building blocks of the biologically active substance or therapeutic agent to obtain said biologically active substance or therapeutic. A product created by this process is also provided herein. The invention is particularly useful to create T-20 and T-1249 therapeutics.