卡西碱 | 477-89-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 中文名称: 卡西碱
• 英文名称: casimiroin
• 英文别名: 6-methoxy-9-methyl-[1,3]dioxolo[4,5-h]quinolin-8-one
• CAS: 477-89-4
• 化学式: C₁₂H₁₁NO₄
• 分子量: 233.224
• InChiKey: DPXXJCMMMXZVSW-UHFFFAOYSA-N

物化性质

• 熔点：
  203°
• 沸点：
  375.46°C (rough estimate)
• 密度：
  1.2697 (rough estimate)
• 物理描述：
  Solid

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  48
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  卡西碱 在 四氢呋喃 、 lithium aluminium tetrahydride 作用下， 生成 9-methyl-6,7,8,9-tetrahydro-[1,3]dioxolo[4,5-h]quinolin-6-ol
  参考文献：
  名称：

  The Constituents of Casimiroa edulis Llave et Lex. III.¹ The Structure of Casimiroin²

  摘要：

  DOI：

  10.1021/ja01580a056
• 作为产物：
  描述：

  4-isocyanato-benzo[1,3]dioxole 在 盐酸 、 sodium hydroxide 作用下， 以 甲醇 、 乙醚 、 硝基甲烷 为溶剂， 生成 卡西碱
  参考文献：
  名称：

  杂环化合物-V：辣椒素的合成

  摘要：

  将乙氧基乙炔加到异氰酸2，3-亚甲基二氧基苯基酯中，得到4-乙氧基-7，8-亚甲基二氧基-2-喹诺酮。喹诺酮的N-甲基化，然后乙氧基水解，并用重氮甲烷处理，得到4-甲氧基-1-甲基-7,8-亚甲基二氧基-2-喹诺酮。该反应序列提供了天然存在的化合物卡西罗林的合成。

  DOI：

  10.1016/s0040-4020(01)99173-2

文献信息

• [EN] PROTEOSTASIS REGULATORS FOR TREATING CYSTIC FIBROSIS AND OTHER PROTEIN MISFOLDING DISEASES<br/>[FR] RÉGULATEURS DE PROTÉOSTASIE POUR LE TRAITEMENT DE LA MUCOVISCIDOSE ET AUTRES MALADIES DE MAUVAIS REPLIEMENT DES PROTÉINES
  申请人：PROTEOSTASIS THERAPEUTICS INC

  公开号：WO2012154880A1

  公开（公告）日：2012-11-15

  The present invention is directed to compounds of Formulae (Ia-Ib), (Ila-IId), (Illa- Illb), (IV), (V), (VI), (Vlla-VIIc), (VIII), (IXa-IXb), (Xa-Xb), (XIa-XIb) and (Xlla-XIIb), pharmaceutical compositions thereof and methods of use thereof in the treatment of conditions associated with a dysfunction in proteostasis.

  本发明涉及式(Ia-Ib)、(IIa-IId)、(IIIa-IIIb)、(IV)、(V)、(VI)、(VIla-VIIc)、(VIII)、(IXa-IXb)、(Xa-Xb)、(XIa-XIb)和(XIIa-XIIb)的化合物，以及这些化合物的药物组合物和在治疗与蛋白质稳态失调相关的疾病中的使用方法。
• [EN] QUINOLONES AS INHIBITORS OF CLASS IV BROMODOMAIN PROTEINS<br/>[FR] QUINOLONES À TITRE D'INHIBITEURS DE PROTÉINES À BROMODOMAINES DE CLASSE IV
  申请人：UCL BUSINESS PLC

  公开号：WO2016034512A1

  公开（公告）日：2016-03-10

  The present invention provides compounds of formula (I) as described herein and pharmaceutically acceptable salts, hydrates and solvates thereof for use in medicine, for example in the treatment of acute myeloid leukaemia:

  本发明提供了如下所述的化合物(I)及其药用可接受的盐、水合物和溶剂合物，用于医学上的应用，例如用于治疗急性髓样白血病：
• Process for production of vinyl chloride polymer
  申请人：Shin-Etsu Chemical Co., Ltd.

  公开号：EP0172427A2

  公开（公告）日：1986-02-26

  This process is a process for production of a vinyl chloride polymer by suspension polymerization or emulsion polymerization of vinyl chloride monomer or a mixture of vinyl chloride monomer with a vinyl monomer copolymerizable with said vinyl chloride monomer in an aqueous medium, characterized in that the polymerization is carried out in a polymerizer, the inner wall surface and portions of the auxiliary equipment thereof which may come into contact with the monomer during polymerization being previously coated with a scaling preventive comprising at least one selected from dyes, pigments and aromatic or heterocyclic compounds having at least 5 conjugated π bonds, while controlling the chloride ion concentration in the reaction mixture to not higher than 100 ppm. According to said process, scaling onto the inner wall surface of a polymerizer, etc. during polymerization can be prevented effectively and surely.

  该工艺是通过氯乙烯单体或氯乙烯单体与可与所述氯乙烯单体共聚的乙烯基单体混合物在水介质中进行悬浮聚合或乳液聚合来生产氯乙烯聚合物的工艺，其特征在于聚合是在聚合器中进行的、内壁表面及其辅助设备中可能在聚合过程中与单体接触的部分事先涂上一层防垢剂，该防垢剂至少包括一种选自染料、颜料和至少有 5 个共轭 π 键的芳香族或杂环化合物的防垢剂，同时控制反应混合物中的氯离子浓度不高于 100 ppm。根据上述工艺，可有效、可靠地防止聚合过程中聚合器等内壁表面结垢。
• Polymerization process characterized by a two layer coating against scale formation deposited using a steam carrier
  申请人：SHIN-ETSU CHEMICAL CO., LTD.

  公开号：EP0934955A1

  公开（公告）日：1999-08-11

  An improved process for producing a polymer by polymerizing a monomer having an ethylenic double bond in a polymerization vessel having a polymer scale preventive coating film on its inner wall surfaces, etc. is provided. The coating film is formed by coating a first coating liquid containing a compound selected from the group consisting of an aromatic compound having 5 or more conjugated π bonds and a heterocyclic compound having 5 or more conjugated π bonds, and then coating a second coating liquid on the first layer. The first and second coating liquids are applied by means of steam as a carrier. The second layer has a surface having a contact angle to water of less than 60° after its surface has been brought into contact with a solution of mixture of water and a vinyl chloride monomer in a weight ratio of 1:1, at 50°C for 1 hour. This process can shorten the time for forming the coating film to improve productivity, can improve the effect of preventing adhesion of polymer scale, can make colored particles less mix into polymer products obtained by this process, can lessen fish eyes and initial discoloring of formed products and can improve the quality of polymeric products and their formed or molded products.

  本发明提供了一种通过在聚合容器中聚合具有乙烯双键的单体来生产聚合物的改进工艺，该聚合容器的内壁表面等处具有聚合物防垢涂膜。该涂膜是通过涂覆第一涂覆液形成的，第一涂覆液含有选自具有 5 个或更多共轭 π 键的芳香族化合物和具有 5 个或更多共轭 π 键的杂环化合物的一组化合物，然后在第一层上涂覆第二涂覆液。第一种和第二种涂覆液通过蒸汽作为载体进行涂覆。第二层表面与水和氯乙烯单体重量比为 1:1 的混合物溶液在 50°C 下接触 1 小时后，其表面与水的接触角小于 60°。这种工艺可以缩短涂膜的形成时间，从而提高生产率；可以提高防止聚合物鳞片附着的效果；可以使有色颗粒较少地混入通过这种工艺获得的聚合物产品中；可以减少成型产品的鱼眼和初期褪色现象；可以提高聚合物产品及其成型或模塑产品的质量。
• Process for producing a polymer by polymerization of a monomer having an ethylenic double bond
  申请人：SHIN-ETSU CHEMICAL CO., LTD.

  公开号：EP1063242A1

  公开（公告）日：2000-12-27

  A process for producing a polymer by polymerizing in a polymerization vessel a monomer having an ethylenic double bond is provided. In this process, the polymerization vessel has a polymer scale preventive coating film on its inner wall surfaces and other surfaces with which the monomer comes into contact during polymerization. The coating film is formed by coating a first coating liquid containing a compound selected from the group consisting of an aromatic compound having 5 or more conjugated π bonds and a heterocyclic compound having 5 or more conjugated π bonds and a second coating liquid containing at least one hydrophilic compound selected from the group consisting of a water-soluble polymeric compound, an inorganic colloid, an inorganic salt and an acid; the first coating liquid and the second coating liquid being simultaneously coated by means of steam as a carrier. This process can shorten the time for forming coating films of scale preventive agents to improve productivity, can improve the effect of preventing scales, can make colored particles less mix into polymer products obtained by this process, can lessen fish eyes and initial discoloring of formed products and can improve the quality of polymeric products and their formed or molded products.

  提供了一种通过在聚合容器中聚合具有乙烯双键的单体来生产聚合物的工艺。在该工艺中，聚合容器的内壁表面和聚合过程中单体接触的其他表面上有一层聚合物防垢涂膜。涂膜是通过涂覆第一涂覆液和第二涂覆液形成的，第一涂覆液含有一种选自具有 5 个或更多共轭 π 键的芳香族化合物和具有 5 个或更多共轭 π 键的杂环化合物的化合物，第二涂覆液含有至少一种选自水溶性高分子化合物、无机胶体、无机盐和酸的亲水性化合物；第一涂覆液和第二涂覆液通过蒸汽作为载体同时涂覆。这种工艺可以缩短防垢剂形成涂膜的时间以提高生产率，可以提高防垢效果，可以使有色颗粒较少地混入通过该工艺获得的聚合物产品中，可以减少成型产品的鱼眼和初始变色，可以提高聚合物产品及其成型或模塑产品的质量。