2-chlorotrityl bromoacetate | 957494-32-5

• 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: 2-chlorotrityl bromoacetate
• 英文别名: [(2-Chlorophenyl)-diphenylmethyl] 2-bromoacetate
• CAS: 957494-32-5
• 化学式: C₂₁H₁₆BrClO₂
• 分子量: 415.714
• InChiKey: RZBSBKFMWFPRCB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.2
• 重原子数：
  25
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  26.3
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  Fmoc-L-丙氨酸 、 2-chlorotrityl bromoacetate 、 Fmoc-L-苯丙氨酸 、 Fmoc-L-天冬氨酸 beta-叔丁酯 、 Fmoc-O-叔丁基-L-谷氨酸 、 Fmoc-N'-甲基三苯甲基-L-赖氨酸 在 1-羟基苯并三唑 、 N,N'-二异丙基碳二亚胺 、 哌啶 作用下， 反应 1.17h， 生成 N2-L-aspartyl-L-glutamyl-L-phenylalanyl-N6-(carboxymethyl)-L-lysyl-L-alanyl-L-aspartyl-L-glutamic acid
  参考文献：
  名称：

  Advanced Glycation End Product Recognition by the Receptor for AGEs

  摘要：

  Nonenzymatic protein glycation results in the formation of advanced glycation end products (AGEs) that are implicated in the pathology of diabetes, chronic inflammation, Alzheimer's disease, and cancer. AGEs mediate their effects primarily through a receptor-dependent pathway in which AGEs bind to a specific cell surface associated receptor, the Receptor for AGEs (RAGE). NE-carboxy-methyllysine (CML) and N-epsilon-carboxy-ethyl-lysine (CEL), constitute two of the major AGE structures found in tissue and blood plasma, and are physiological ligands of RAGE. The solution structure of a CEL-containing peptide-RAGE V domain complex reveals that the carboxyethyl moiety fits inside a positively charged cavity of the V domain. Peptide backbone atoms make specific contacts with the V domain. The geometry of the bound CEL peptide is compatible with many CML (CEL)-modified sites found in plasma proteins. The structure explains how such patterned ligands as CML (CEL)-proteins bind to RAGE and contribute to RAGE signaling.

  DOI：

  10.1016/j.str.2011.02.013
• 作为产物：
  描述：

  氯代(邻氯苯基)二苯基甲烷 、 溴乙酸 在 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 1.0h， 生成 2-chlorotrityl bromoacetate
  参考文献：
  名称：

  Advanced Glycation End Product Recognition by the Receptor for AGEs

  摘要：

  Nonenzymatic protein glycation results in the formation of advanced glycation end products (AGEs) that are implicated in the pathology of diabetes, chronic inflammation, Alzheimer's disease, and cancer. AGEs mediate their effects primarily through a receptor-dependent pathway in which AGEs bind to a specific cell surface associated receptor, the Receptor for AGEs (RAGE). NE-carboxy-methyllysine (CML) and N-epsilon-carboxy-ethyl-lysine (CEL), constitute two of the major AGE structures found in tissue and blood plasma, and are physiological ligands of RAGE. The solution structure of a CEL-containing peptide-RAGE V domain complex reveals that the carboxyethyl moiety fits inside a positively charged cavity of the V domain. Peptide backbone atoms make specific contacts with the V domain. The geometry of the bound CEL peptide is compatible with many CML (CEL)-modified sites found in plasma proteins. The structure explains how such patterned ligands as CML (CEL)-proteins bind to RAGE and contribute to RAGE signaling.

  DOI：

  10.1016/j.str.2011.02.013

文献信息

• [EN] TRIAZINE COMPOUNDS, COMPOSITIONS AND SYNTHESIS<br/>[FR] COMPOSÉS DE TRIAZINE, COMPOSITIONS ET SYNTHÈSE
  申请人：CTXT PTY LTD

  公开号：WO2016070241A1

  公开（公告）日：2016-05-12

  The present invention generally relates to triazine compounds, methods for preparing triazine compounds and compositions comprising triazine compounds. The present invention also relates to triazine compounds and their use as intermediates in methods for preparing target triazine compounds, which enables access to suitable triazine based anti-cancer agents.

  本发明通常涉及三嗪化合物、制备三嗪化合物的方法以及包含三嗪化合物的组合物。本发明还涉及三嗪化合物及其用途作为制备目标三嗪化合物的中间体，从而可以获得适用于三嗪基抗癌剂的三嗪化合物。
• Insulinotropic peptide synthesis using solid and solution phase combination techniques
  申请人：Chen Lin

  公开号：US20090292108A1

  公开（公告）日：2009-11-26

  The present invention relates to the preparation of insulinotropic peptides that are synthesized using a solid and solution phase (“hybrid”) approach. Generally, the approach includes synthesizing three different peptide intermediate fragments using solid phase chemistry. Solution phase chemistry is then used to add additional amino acid material to the third fragment which is then coupled to the second fragment and then the first fragment in solution. Alternatively, a different second fragment is coupled to the first fragment in the solid phase. Then, solution phase chemistry is then used to add additional amino acid material to a different third fragment. Subsequently, this different third fragment is coupled to the coupled first and different second fragment in the solution phase. The use of a pseudoproline in one of the fragments eases solid phase synthesis of that fragment and also eases subsequent solution phase coupling of this fragment to the other fragments. The present invention is very useful for forming insulinotropic peptides such as GLP-1(7-36) and its natural and non-natural counterparts.

  本发明涉及使用固相和溶液相（“混合”）方法合成胰岛素促分泌肽的制备。通常，该方法包括使用固相化学合成三种不同的肽中间片段。然后，使用溶液相化学将额外的氨基酸材料添加到第三个片段中，然后在溶液中将第三个片段耦合到第二个片段，然后再将第一片段耦合到溶液中。或者，在固相中将不同的第二个片段耦合到第一片段。然后，使用溶液相化学将额外的氨基酸材料添加到不同的第三个片段中。随后，将这个不同的第三个片段耦合到耦合的第一个和不同的第二个片段中的溶液相中。在其中一个片段中使用假丝氨酸可以减轻该片段的固相合成，并且还可以减轻该片段与其他片段的随后溶液相耦合。本发明非常有用，可用于形成胰岛素促分泌肽，例如GLP-1（7-36）及其天然和非天然对应物。
• Peptides and their use in food and beverage
  申请人：The Folger Coffee Company

  公开号：US10005816B2

  公开（公告）日：2018-06-26

  Described herein is a peptide with an amino acid sequence comprising a Leu-Leu moiety. Also described is a composition having a mixture of such peptides, and foods and beverages containing such compositions including, for example, roast and ground coffee, coffee brew, coffee creamer, and tea. The addition of one or more of these peptide(s) to coffee brews made from instant coffee, liquid coffee concentrate, or decaf coffee demonstrates that these peptides improve the taste profile of such coffee brews.

  本文所描述的是一种肽，其氨基酸序列包含一个Leu-Leu分子。还描述了具有这种多肽混合物的组合物，以及含有这种组合物的食品和饮料，例如包括烘焙和研磨咖啡、咖啡冲剂、咖啡奶精和茶。在速溶咖啡、液态浓缩咖啡或无咖啡因咖啡制成的咖啡冲剂中加入一种或多种此类肽，表明这些肽可改善此类咖啡冲剂的口味。
• High molecular weight biodegradable gelatin-doxorubicin conjugate
  申请人：UNIVERSITY OF THE SCIENCES IN PHILADELPHIA

  公开号：US10265413B2

  公开（公告）日：2019-04-23

  Disclosed herein are high molecular weight compounds comprising gelatin and doxorubicin, where the gelatin is covalently linked to doxorubicin through a cleavable linker. The cleavable linker can be cleaved under appropriate physiological conditions, and thus lead to the freeing of doxorubicin. The free doxorubicin can then exert its cytotoxic effects on cancer cells. Disclosed herein are methods of making the high molecular weight gelatin-doxorubicin conjugates and methods of use of the same.

  本文公开了由明胶和多柔比星组成的高分子量化合物，其中明胶通过可裂解连接体与多柔比星共价连接。可裂解连接体可在适当的生理条件下被裂解，从而导致多柔比星的游离。游离的多柔比星可对癌细胞发挥细胞毒性作用。本文公开了高分子量明胶-多柔比星共轭物的制造方法及其使用方法。
• Synthesis using peptide intermediate fragments
  申请人：Khatri N. Hiralal

  公开号：US20060173163A1

  公开（公告）日：2006-08-03

  Methods for the solid phase synthesis of T-1249 peptides and peptide intermediates, in particular methods involving synthesizing T-1249 peptide intermediates at low loading factors to produce products having excellent purity and yield.

  T-1249 多肽和多肽中间体的固相合成方法，特别是以低负载因子合成 T-1249 多肽中间体以生产纯度和收率极高的产品的方法。