Cholesterolformate | 4351-55-7

• 物质功能分类: 化学试剂 - 有机试剂 - 酯类
• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 英文名称: Cholesterolformate
• 英文别名: [(8S,9S,10R,13R,14S,17R)-10,13-dimethyl-17-[(2R)-6-methylheptan-2-yl]-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-yl] formate
• CAS: 4351-55-7
• 化学式: C₂₈H₄₆O₂
• 分子量: 414.7
• InChiKey: YEYCQJVCAMFWCO-ULEPMCFASA-N

物化性质

• 熔点：
  95 °C
• 沸点：
  487.1±15.0 °C(Predicted)
• 密度：
  1.00±0.1 g/cm3(Predicted)
• LogP：
  10.298 (est)

计算性质

• 辛醇/水分配系数(LogP)：
  9.1
• 重原子数：
  30
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  26.3
• 氢给体数：
  0
• 氢受体数：
  2

安全信息

• 危险品标志：
  Xi
• WGK Germany：
  3
• 安全说明：
  S26,S39
• 危险类别码：
  R41

反应信息

• 作为产物：
  描述：

  2-氧代吡啶-1-甲醛 、 胆甾-5-烯-3-醇 以93%的产率得到
  参考文献：
  名称：

  EFFENBERGER F.; KEIL M.; BESSEY E., CHEM. BER., 1980, 113, NO 6, 2110-2119

  摘要：

  DOI：

文献信息

• [EN] CHOLESTEROL/BILE ACID/BILE ACID DERIVATIVE-MODIFIED THERAPEUTIC ANTI-CANCER DRUGS<br/>[FR] MEDICAMENTS ANTICANCEREUX THERAPEUTIQUES MODIFIES PAR LE CHOLESTEROL/L'ACIDE BILIAIRE/LES DERIVES D'ACIDE BILIAIRE
  申请人：SONUS PHARMA INC

  公开号：WO2005118612A1

  公开（公告）日：2005-12-15

  Cholesterol-modified anti-cancer therapeutic drug compounds, bile-acid-modified anti-cancer therapeutic drug compounds, and bile-acid-derivative-modified anti-cancer therapeutic drug compounds; emulsion, microemulsion, and micelle formulations that include the compounds, methods for administering the compounds and formulations; and methods for treating cancer using the compounds and formulations.

  胆固醇修饰的抗癌治疗药物化合物，胆酸修饰的抗癌治疗药物化合物，以及胆酸衍生物修饰的抗癌治疗药物化合物；包括这些化合物的乳剂、微乳剂和胶束配方，用于给药这些化合物和配方的方法；以及使用这些化合物和配方治疗癌症的方法。
• APOLIPOPROTEIN NANODISCS WITH TELODENDRIMER
  申请人：The Regents of The University of California

  公开号：US20130165636A1

  公开（公告）日：2013-06-27

  The present invention provides a nanodisc with a membrane scaffold protein. The nanodisc includes a membrane scaffold protein, a telodendrimer and a lipid. The membrane scaffold protein can be apolipoprotein. The telodendrimer has the general formula PEG-L-D-(R) n , wherein D is a dendritic polymer; L is a bond or a linker linked to the focal point group of the dendritic polymer; each PEG is a poly(ethylene glycol) polymer; each R is and end group of the dendritic polymer, or and end group with a covalently bound hydrophobic group, hydrophilic group, amphiphilic compound, or drug; and subscript n is an integer from 2 to 20. Cell free methods of making the nanodiscs are also provided.

  本发明提供了一种具有膜支架蛋白的纳米盘。该纳米盘包括膜支架蛋白、端酯聚合物和脂质。膜支架蛋白可以是载脂蛋白。端酯聚合物具有通式PEG-L-D-(R)n，其中D是树枝状聚合物；L是与树枝状聚合物的焦点基团连接的键或连接物；每个PEG是聚乙二醇聚合物；每个R是树枝状聚合物的末端基团，或具有共价结合的疏水基团、亲水基团、两性化合物或药物的末端基团；下标n是2到20之间的整数。还提供了制备纳米盘的无细胞方法。
• Telodendrimers with enhanced drug delivery
  申请人：The Regents of the University of California

  公开号：US10406233B2

  公开（公告）日：2019-09-10

  The present invention provides amphiphilic telodendrimers that aggregate to form nanocarriers characterized by a hydrophobic core and a hydrophilic exterior. The nanocarrier core may include amphiphilic functionality such as cholic acid or cholic acid derivatives, and the exterior may include branched or linear poly(ethylene glycol) segments. Nanocarrier cargo such as hydrophobic drugs and other materials may be sequester in the core via non-covalent means or may be covalently bound to the telodendrimer building blocks. Telodendrimer structure may be tailored to alter loading properties, interactions with materials such as biological membranes, and other characteristics.

  本发明提供了一种两性端树脂，它们聚集形成纳米载体，具有疏水核心和亲水外层的特点。纳米载体核心可能包括两性功能，如胆酸或胆酸衍生物，外层可能包括分支或线性聚乙二醇片段。纳米载体货物，如疏水药物和其他材料，可以通过非共价手段被封存在核心中，也可以与两性端树脂构建块共价结合。两性端树脂结构可以定制以改变装载特性、与生物膜等材料的相互作用以及其他特性。
• TELODENDRIMERS WITH ENHANCED DRUG DELIVERY
  申请人：The Regents of the University of California

  公开号：US20140363371A1

  公开（公告）日：2014-12-11

  The present invention provides amphiphilic telodendrimers that aggregate to form nanocarriers characterized by a hydrophobic core and a hydrophilic exterior. The nanocarrier core may include amphiphilic functionality such as cholic acid or cholic acid derivatives, and the exterior may include branched or linear poly(ethylene glycol) segments. Nanocarrier cargo such as hydrophobic drugs and other materials may be sequester in the core via non-covalent means or may be covalently bound to the telodendrimer building blocks. Telodendrimer structure may be tailored to alter loading properties, interactions with materials such as biological membranes, and other characteristics.

  本发明提供了一种两亲性末端树状高聚物，它们聚集形成纳米载体，具有疏水核和亲水外壳的特征。纳米载体核可以包括胆酸或胆酸衍生物等两亲性功能，外壳可以包括分支或线性聚乙二醇片段。疏水药物和其他材料等纳米载体货物可以通过非共价手段被隔离在核内，也可以被共价地结合到末端树状高聚物建筑块上。末端树状高聚物结构可以被调整以改变装载性能、与生物膜等材料的相互作用和其他特性。
• Process for the preparation of active-type vitamin D3 compounds and of the cholesta-5,7-diene precursors, and products so obtained
  申请人：TEIJIN LIMITED

  公开号：EP0028484A1

  公开（公告）日：1981-05-13

  The present invention relates to a novel process for the preparation of active-type vitamin D3 compounds and their intermediates. In accordance with the present invention, a large amount of an active-type vitamin D3 compound, for example 1α-hydroxycholecalciferol, 1α,25-dihydrox- ycholecalciferol and the like, is efficiently prepared with high industrial advantage by a novel process which comprises (i) reacting hydroxycholesta-5-enes having the hydroxyl groups protected with lower alkoxycarbonyl groups as a starting material with an allylic brominating agent and a dehydrobrominating agent to prepare the corresponding hydroxycholesta-5,7-dienes, (ii) exposing the hydroxycholesta-5,7-dienes to ultraviolet irradiation or to a combination of the irradiation with thermal isomerization to obtain a mixture of the unreacted hydroxycholesta-5,7-dienes and previtamin D3 compounds or a mixture of the unreacted hydroxycholesta-5,7-dienes and the protected active-type vitamin D, compounds, (iii) separating the mixture into the unreacted hydroxycholesta-5,7-dienes and previtamin D3 compounds or the protected active-type vitamin D3 compounds, (iv) recycling the unreacted hydroxycholesta-5,7-dienes for reuse and (v) thermally isomerizing the remaining compounds and/or splitting off the protective groups. The process of the invention is of very high industrial value, capable of simple operation and adaptable to large scale commercial production.

  本发明涉及一种制备活性型维生素 D3 化合物及其中间体的新工艺。根据本发明，大量活性型维生素 D3 化合物，例如 1α-羟基胆钙化醇、1α,25-二羟基胆钙化醇等、该工艺包括：(i) 以羟基被低级烷氧羰基保护的羟基胆甾烷-5-烯为起始原料，与烯丙基溴化剂和脱氢溴化剂反应，制备相应的羟基胆甾烷-5,7-二烯；(ii) 将羟基胆甾烷-5、(ii) 将羟基胆甾烷-5,7-二烯置于紫外线辐照下，或将辐照与热异构化相结合，以获得未反应的羟基胆甾烷-5,7-二烯与前维生素 D3 化合物的混合物，或未反应的羟基胆甾烷-5,7-二烯与受保护的活性型维生素 D 化合物的混合物、(iii) 将混合物分离为未反应的羟基胆甾烷-5,7-二烯和前维生素 D3 化合物或受保护的活性型维生素 D3 化合物， (iv) 回收未反应的羟基胆甾烷-5,7-二烯以供再利用， (v) 对剩余化合物进行热异构化和/或分离保护基团。本发明的工艺具有极高的工业价值，操作简单，可适应大规模商业生产。