4-(三苯甲游基氧基)苯甲醛 | 892112-24-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 中文名称: 4-(三苯甲游基氧基)苯甲醛
• 中文别名: 4-(三苯甲基氧基)苯甲醛
• 英文名称: 4-trityloxy-benzaldehyde
• 英文别名: 4-(Trityloxy)benzaldehyde；4-trityloxybenzaldehyde
• CAS: 892112-24-2
• 化学式: C₂₆H₂₀O₂
• 分子量: 364.444
• InChiKey: YXWHPUQQTIIFGZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6
• 重原子数：
  28
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.04
• 拓扑面积：
  26.3
• 氢给体数：
  0
• 氢受体数：
  2

安全信息

• 海关编码：
  2912499000
• 储存条件：
  温度：2-8°C，保持在惰性气体氛围中。

反应信息

• 作为反应物：
  描述：

  4-(三苯甲游基氧基)苯甲醛 在 氢氧化钾 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 反应 1.5h， 生成 4-trityloxyphenyldiazomethane
  参考文献：
  名称：

  海洋吡咯并喹啉生物碱的吡唑类似物的合成和抗肿瘤特性：若卡因和tsitsikammamines。

  摘要：

  已经合成了一系列海洋生物碱wakayin和tsitsikammamines A和B的氮杂类似物。所使用的策略是基于[3 + 2]环加成反应，其中涉及3-乙胺-吲哚-4,7-二酮和不同的重氮试剂。在体外评估了所有化合物对五种不同癌细胞系的抗增殖活性以及它们对拓扑异构酶同工酶I和II的抑制作用。一些化合物以与喜树碱和依托泊苷相当的浓度抑制拓扑异构酶I和/或II催化超螺旋DNA的松弛。它们中只有少数表现出细胞毒性活性，IC50值在微摩尔范围内。

  DOI：

  10.1021/jm051247f
• 作为产物：
  描述：

  三苯基氯甲烷 、 对羟基苯甲醛 在 4-二甲氨基吡啶 、 三乙胺 作用下， 以 四氢呋喃 为溶剂， 以92%的产率得到4-(三苯甲游基氧基)苯甲醛
  参考文献：
  名称：

  海洋吡咯并喹啉生物碱的吡唑类似物的合成和抗肿瘤特性：若卡因和tsitsikammamines。

  摘要：

  已经合成了一系列海洋生物碱wakayin和tsitsikammamines A和B的氮杂类似物。所使用的策略是基于[3 + 2]环加成反应，其中涉及3-乙胺-吲哚-4,7-二酮和不同的重氮试剂。在体外评估了所有化合物对五种不同癌细胞系的抗增殖活性以及它们对拓扑异构酶同工酶I和II的抑制作用。一些化合物以与喜树碱和依托泊苷相当的浓度抑制拓扑异构酶I和/或II催化超螺旋DNA的松弛。它们中只有少数表现出细胞毒性活性，IC50值在微摩尔范围内。

  DOI：

  10.1021/jm051247f

文献信息

• Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof
  申请人：CoCensys, Inc.

  公开号：US20020061886A1

  公开（公告）日：2002-05-23

  This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: 1 or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R 1 , R 21 , R 22 and R 23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R 22 and R 23 , together with the N, form a heterocycle; A 1 and A 2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR 24 , CR 25 R 26 , C(O), NR 24 C(O), C(O)NR 24 , SO, SO 2 or a covalent bond; where R 24 , R 25 and R 26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl. The invention also is directed to the use of carbocycle and heterocycle substituted semicarbazones and thiosemicarbazones for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), for the treatment and prevention of otoneurotoxicity and eye diseases involving glutamate toxicity and for the treatment, prevention or amelioration of pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy and urinary incontinence.

  这项发明涉及由式I表示的含有碳环和杂环取代的半卡巴松和硫代半卡巴松： 1 或其药学上可接受的盐或前药，其中： Y为氧或硫；R 1 ，R 21 ，R 22 和R 23 独立地为氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基；或R 22 和R 23 ，与N一起形成一个杂环；A 1 和A 2 独立地为芳基，杂芳基，饱和或部分不饱和的碳环或饱和或部分不饱和的杂环，其中任何一个可选择地被取代；X为O、S、NR 24 、CR 25 R 26 、C(O)、NR 24 C(O)、C(O)NR 24 、SO、SO 2 或共价键；其中R 24 ，R 25 和R 26 独立地为氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基。该发明还涉及利用含有碳环和杂环取代的半卡巴松和硫代半卡巴松治疗全脑和局部缺血后的神经损伤，治疗或预防神经退行性疾病如肌萎缩侧索硬化症（ALS），治疗和预防耳神经毒性和涉及谷氨酸毒性的眼病，以及治疗、预防或改善疼痛，作为抗癫痫药，作为抗躁狂抑郁药，作为局部麻醉药，作为抗心律失常药，以及治疗或预防糖尿病性神经病变和尿失禁。
• New phosphorylating reagents for deoxyribonucleosides and oligonucleotides
  作者：Valeria Romanucci、Armando Zarrelli、Annalisa Guaragna、Cinzia Di Marino、Giovanni Di Fabio

  DOI：10.1016/j.tetlet.2017.02.034

  日期：2017.3

  New phosphorylating reagents 1 and 2 were prepared in three steps from 4-hydroxybenzaldehyde. They showed good efficiency in the solid phase synthesis of 5′-phosphate monoester nucleosides. End-phosphate DNA sequence synthesis demonstrated the efficiency of the new reagents (1 and 2) according to the general procedure of automated DNA synthesis. The oxidation of P(III) to P(V) and the removal of benzyl

  由4-羟基苯甲醛分三步制备新的磷酸化试剂1和2。他们在固相合成5'-磷酸单酯核苷中显示出良好的效率。根据自动DNA合成的一般程序，磷酸末端DNA序列合成证明了新试剂（1和2）的效率。通过用0.02 MI 2 /吡啶/ H 2 O溶液处理，在单个步骤中实现了将P（III）氧化为P（V）并去除苄基保护基。由于采用一锅法处理，因此可以使用磷酸化试剂（1和2），用于合成对碱基敏感的ODN。试剂1和2在磷酸化试剂中是独特的。
• 一种紫檀芪的合成方法
  申请人：珠海市柏瑞医药科技有限公司

  公开号：CN116813454A

  公开（公告）日：2023-09-29

  本发明涉及化学合成领域，公开一种紫檀芪的合成方法，包括以下步骤：化合物A和4‑(三苯甲氧基)‑苯乙烯进行Heck反应得2‑4‑[(E)‑2‑(3,5‑二甲氧基苯基)‑1‑乙烯基]苯氧基三苯，化合物A为3,5‑二甲氧基苯甲酰氯、3,5‑二甲氧基苯甲酰溴、3,5‑二甲氧基氯苯、3,5‑二甲氧基苯溴苯、3,5‑二甲氧基碘苯的一种。本发明提供一种通过Heck反应构建单一构型紫檀芪的方法，转化率高，且容易操作。
• The use of carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones as sodium channel blockers
  申请人：Euro-Celtique S.A.

  公开号：EP1568690A1

  公开（公告）日：2005-08-31

  This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by formula (I), or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl. The invention is also directed to the use of carbocycle and heterocycle substituted semicarbazones and thiosemicarbazones for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyiotrophic lateral sclerosis (ALS), for the treatment and prevention of otoneurotoxicity and eye diseases involving glutamate toxicity and for the treatment, prevention or amelioration of pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy and urinary incontinence.

  本发明涉及式(I)代表的碳环和杂环取代的半咔唑酮和硫代咔唑酮，或其药学上可接受的盐或原药，其中：Y是氧或硫；R1、R21、R22和R23独立地是氢、烷基、环烷基、烯基、炔基、卤代烷基、芳基、氨基烷基、羟基烷基、烷氧基烷基或羧基烷基；或R22和R23与N一起形成杂环；A1和A2独立地是芳基、杂芳基、饱和或部分不饱和碳环或饱和或部分不饱和杂环，其中任何一个都被任选取代；X是一个或O、S、NR24、CR25R26、C(O)、NR24C(O)、C(O)NR24、SO、SO2或共价键；其中R24、R25和R26独立地是氢、烷基、环烷基、烯基、炔基、卤代烷基、芳基、氨基烷基、羟基烷基、烷氧基烷基或羧基烷基。本发明还涉及碳环和杂环取代的半咔唑酮和硫代咔唑酮用于治疗全局性和局灶性缺血后的神经元损伤，治疗或预防神经退行性疾病，如肌萎缩性脊髓侧索硬化症（ALS）、用于治疗和预防耳神经毒性和涉及谷氨酸毒性的眼部疾病，用于治疗、预防或改善疼痛，用作抗惊厥药、抗躁狂抑制剂、局部麻醉剂、抗心律失常药，以及用于治疗或预防糖尿病神经病变和尿失禁。
• Synthesis and Structure−Affinity Relationships of Novel Dibenzylideneacetone Derivatives as Probes for β-Amyloid Plaques
  作者：Mengchao Cui、Masahiro Ono、Hiroyuki Kimura、Boli Liu、Hideo Saji

  DOI：10.1021/jm101404k

  日期：2011.4.14

  A new and extensive set of dibenzylideneacetone derivatives was synthesized and screened for affinity toward A beta(1-42) aggregates. Structure-activity relationships revealed the binding of dibenzylideneacetones to be affected by various substituents. The introduction of a substituent group in the ortho position reduced or abolished the binding. However, the para position was highly tolerant of sterically demanding substitutions. Three radioiodinated ligands (6, 70, and 71) and two F-18 fluoro-pegylated (FPEG) ligands (83 and 85) were prepared, all of which displayed high affinity folr A beta(1-42) aggregates (K-i ranging from 0.9 to 7.0 nM). In biodistribution experiments, they exhibited good initial penetration (1.59, 4.68, 4.56, 4.13, and 5.15% ID/g, respectively, at 2 min) of and fast clearance from the brain. Autoradiography with sections of postmortem AD brain and transgenic mouse brain confirmed the high affinity of these tracers. These preliminary results strongly suggest the dibenzylideneacetone structure to be a potential new scaffold for beta-amyloid imaging probes.