homochelidonine | 857020-96-3

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 苯并菲啶生物碱
• 英文名称: homochelidonine
• 英文别名: Homoquelidonin；(4bR)-1,2-dimethoxy-12-methyl-(4br,11bc)-4b,5,6,11b,12,13-hexahydro-[1,3]dioxolo[4',5':4,5]benzo[1,2-c]phenanthridin-5t-ol；1,2-dimethoxy-12-methyl-4b,5,6,11b,12,13-hexahydro-[1,3]dioxolo[4',5':4,5]benzo[1,2-c]phenanthridin-5-ol；1,2-dimethoxy-12-methyl-5,6,11b,13-tetrahydro-4bH-[1,3]benzodioxolo[5,6-c]phenanthridin-5-ol
• CAS: 857020-96-3
• 化学式: C₂₁H₂₃NO₅
• 分子量: 369.417
• InChiKey: MADYLZJCRKUBIK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  27
• 可旋转键数：
  2
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  60.4
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• Quaternary chelidonine and alkaloid derivatives, process for their preparation and their use in the manufacture of medicaments
  申请人：Nowicky, Wassyl, Dipl.-Ing. DDr.

  公开号：EP1459753A1

  公开（公告）日：2004-09-22

  The invention relates to alkaloid reaction products obtainable in a process wherein alkaloids are reacted with an alkylating agent, preferably thiotepa, whereafter unreacted alkylating agent and other water-soluble compounds are removed from the reaction mixture by washing with water or a suitable aqueous solvent, whereafter the reaction mixture is subjected to a treatment with strong acid, preferably hydrogen chloride (HCl), to precipitate a water soluble salt of the reaction products. The precipitated reaction products comprise at least one quaternary alkaloid derivative and are suitable as drugs for prophylactic or therapeutic application, particularly in the treatment of immunological or metabolic dysfunctions, and cancer.

  该发明涉及一种碱性物质反应产物，可通过一种过程获得，在该过程中，碱性物质与烷基化剂发生反应，优选为硫替巴（thiotepa），随后通过用水或适当的水溶性溶剂洗涤来除去未反应的烷基化剂和其他水溶性化合物，然后将反应混合物经过强酸处理，优选为盐酸（HCl），以沉淀反应产物的水溶性盐。沉淀的反应产物包括至少一种季铵碱性物质衍生物，并适用于用于预防或治疗应用的药物，特别是在免疫或代谢功能障碍以及癌症治疗中。
• [EN] QUATERNARY ALKALOID DERIVATIVES OF CHELIDONIUM MAJUS L<br/>[FR] DERIVES ALCALOIDES QUATERNAIRES DE CHELIDONIUM MAJUS L
  申请人：NOWICKY WASSILI

  公开号：WO2006032380A1

  公开（公告）日：2006-03-30

  The invention relates to alkaloid reaction products obtainable in a process wherein alkaloids are reacted with a derivatizing agent, preferably thiotepa or another one of the compounds listed in Fig.3, whereafter unreacted derivatizing agent and other water-soluble compounds are removed from the reaction mixture by washing with water or a suitable aqueous solvent, whereafter the reaction mixture is subjected to a treatment with strong acid, preferably hydrogen chloride (HCI), to precipitate a water soluble salt of the reaction products. The precipitated reaction products comprise at least one quaternary alkaloid derivative and are suitable as drugs for prophylactic or therapeutic application, particularly in the treatment of immunological or metabolic dysfunctions, and cancer.

  本发明涉及一种碱性物质反应产物，该产物可以在一种过程中获得，该过程中碱性物质与衍生化试剂（优选为硫唑磷或图3中列出的其他化合物之一）反应，然后通过用水或适当的水溶性溶剂洗涤来去除未反应的衍生化试剂和其他水溶性化合物，然后将反应混合物用强酸（优选为盐酸）处理，以沉淀反应产物的水溶性盐。沉淀的反应产物包括至少一种季铵碱衍生物，适用于预防或治疗应用的药物，特别是在免疫或代谢功能障碍和癌症的治疗中。
• Novel compounds and a novel process for their preparation
  申请人：Fagnou Keith

  公开号：US20050014721A1

  公开（公告）日：2005-01-20

  The present invention is directed to a procedure for making an enantiomerically enriched compound containing a hydronaphthalene ring structure. The process involves reacting oxabenzonorbornadienes with nucleophiles using rhodium as a catalyst and in the presence of a phosphine ligand. The compounds synthesized may be used in pharmaceutical preparations for the treatment of a variety of diseases and conditions.

  本发明涉及一种制备含有氢化萘环结构的对映体富集化合物的方法。该过程涉及使用铑作为催化剂，并在膦配体的存在下，将氧化苯并[2,3-c]环辛二烯与亲核试剂反应。合成的化合物可用于制备治疗各种疾病和病况的药物制剂。
• Novel hydronaphthalene compounds, prepared by a rhodium catalysed ring opening reaction in the presence of phosphine ligand
  申请人：AstraZeneca AB

  公开号：EP1498406A1

  公开（公告）日：2005-01-19

  The present invention is directed to a procedure for making an enantiomerically enriched compound containing a hydronaphthalene ring structure. The process involves reacting oxabenzonorbornadienes with nucleophiles using rhodium as a catalyst and in the presence of a phosphine ligand. The compounds synthesized may be used in pharmaceutical preparations for the treatment of a variety of diseases and conditions.

  本发明涉及一种含有氢萘环结构的对映体富集化合物的制造工艺。该过程包括使用铑作为催化剂，在膦配体存在的情况下，使氧杂苯并降冰片二烯与亲核物反应。合成的化合物可用于治疗各种疾病和病症的药物制剂中。
• Zinc chloride unit dose packaging, applicator, and method of use in treating cancer and other skin diseases
  申请人：——

  公开号：US20020081328A1

  公开（公告）日：2002-06-27

  An improved method for the treatment of melanoma and skin diseases which utilizes a zinc chloride fixative mixture is provided. The active ingredients of the fixative mixture include zinc chloride (a deeply penetrating, tissue killing histologic preservative), and the anti-cancer plant alkaloids sanguinarine and chelerythrine. Zinc chloride allows the surgeon to perform a complete conventional surgical excision around and below a melanomatous tumor through painless, bloodless dead tissue, and because the microscopic structures are fixed in place by the zinc chloride, the excised tissue can be examined by a pathologist to confirm complete excision and clearance of the melanoma. Although zinc chloride fixative paste has been shown to be an effective treatment for human skin cancer and melanoma, this treatment has been overlooked by the medical community. The paste is difficult to maintain and complicated to apply to the affected skin. This invention allows the active ingredients of zinc chloride fixative paste to be effectively administered to the skin by providing single-use dose specific storage, application, dressing, and administration systems needed to facilitate the use of topical zinc chloride mixtures and/or zinc chloride pastes in the treatment of melanoma and other skin diseases. Enhanced zinc chloride mixture formulations are described.

  提供了一种利用氯化锌固定剂混合物治疗黑色素瘤和皮肤病的改进方法。该固定剂混合物的有效成分包括氯化锌（一种深层渗透、杀死组织的组织学防腐剂），以及抗癌植物生物碱sanguinarine和chelerythrine。氯化锌可以让外科医生通过无痛、无血的坏死组织，在黑色素瘤周围和下方进行完整的常规手术切除，由于微观结构被氯化锌固定，切除的组织可以由病理学家检查，以确认黑色素瘤的完整切除和清除。尽管氯化锌固定膏已被证明是治疗人类皮肤癌和黑色素瘤的有效方法，但这种治疗方法一直被医学界所忽视。这种糊剂难以保存，而且在患处皮肤上涂抹也很复杂。本发明通过提供一次性使用的特定剂量储存、应用、敷料和给药系统，可将氯化锌固定糊剂的活性成分有效地施用到皮肤上，从而方便使用局部氯化锌混合物和/或氯化锌糊剂治疗黑色素瘤和其他皮肤病。本文介绍了增强型氯化锌混合物配方。