3-(benzhydrylidene-amino)-dihydro-furan-2-one | 88539-65-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 3-(benzhydrylidene-amino)-dihydro-furan-2-one
• 英文别名: 2-diphenylmethyleneamino-γ-butyrolactone；3-[(diphenylmethylene)amino]dihydrofuran-2(3H)-one；3-(benzhydrylideneamino)oxolan-2-one
• CAS: 88539-65-5
• 化学式: C₁₇H₁₅NO₂
• 分子量: 265.312
• InChiKey: PQLBHHRCKIGQAG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  38.7
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-(benzhydrylidene-amino)-dihydro-furan-2-one 、 Cinnamyl bromide 在 正丁基锂 、 lithium 、 二异丙胺 作用下， 以 四氢呋喃 、 hexamethylenephosphoric acid triamide 为溶剂， 生成 2-cinnamyl-2-diphenylmethyleneamino-γ-butyrolactone
  参考文献：
  名称：

  Benzene compound and pharmaceutical use thereof

  摘要：

  一种具有以下结构式的苯化合物##STR1##，其中每个符号如规范中定义；其光学活性异构体或盐，含有该化合物的药物组合物，以及含有该化合物作为活性成分的免疫抑制剂。该化合物、光学活性异构体或盐具有出色的免疫抑制效果，并可用作器官或骨髓移植中发生的排斥反应的抑制剂，以及关节风湿病、特应性湿疹（皮炎）、Beh.cedilla.et氏病、葡萄膜疾病、系统性红斑狼疮、干燥综合征、多发性硬化、重症肌无力、I型糖尿病、内分泌眼病、原发性胆汁性肝硬化、克罗恩病、肾小球肾炎、结节病、牛皮癣、天疱疮、再生障碍性贫血、特发性血小板减少性紫癜、过敏、多动脉炎、进行性系统性硬化、混合结缔组织病、主动脉炎综合征、多发性肌炎、皮肌炎、Wegener氏肉芽肿、溃疡性结肠炎、活动性慢性肝炎、自身免疫性溶血性贫血、Evans氏综合征、支气管哮喘和过敏性鼻炎的预防或治疗。它还可用作抗真菌剂和促进头发生长的刺激剂。

  公开号：

  US05948820A1
• 作为产物：
  描述：

  二苯亚甲基甘氨酸乙酯 、 环氧乙烷 生成 3-(benzhydrylidene-amino)-dihydro-furan-2-one
  参考文献：
  名称：

  CATO, XARUE;IMAMURA, SINDZO

  摘要：

  DOI：

文献信息

• A NEW AND EFFECTIVE AMINOMETHYLATION BY THE USE OF<i>N</i>-(<i>p</i>-TOLUENESULFONYLMETHYL)-<i>p</i>-TOLUENESULFONAMIDE AS AN EQUIVALENT OF METHANIMINE. A CONVENIENT PREPARATION OF PYRROLE COMPOUNDS
  作者：Hideki Kinoshita、Katsuhiko Inomata、Masatoshi Hayashi、Takeshi Kondoh、Hiroshi Kotake

  DOI：10.1246/cl.1986.1033

  日期：1986.6.5

  N-(p-toluenesulfonylmethyl)-p-toluenesulfonamide was treated with base to generate N-methylene-p-toluenesulfonamide which reacted with a variety of nucleophiles forming the corresponding N-tosyl-aminomethylated compounds in good yields. Furthermore, the N-tosyl-aminomethylated acetals thus obtained were converted into the corresponding N-tosylpyrroles with the aid of acid catalyst in excellent yields.

  容易获得的 N-(对甲苯磺酰基甲基)-对甲苯磺酰胺用碱处理以生成 N-亚甲基-对甲苯磺酰胺，其与多种亲核试剂反应以良好的产率形成相应的 N-甲苯磺酰基-氨基甲基化化合物。此外，由此获得的N-甲苯磺酰基-氨基甲基化缩醛在酸催化剂的帮助下以优异的产率转化为相应的N-甲苯磺酰基吡咯。
• Imidazolidin-4-one derivatives useful as anticancer agents
  申请人：Pfizer Inc.

  公开号：US06080769A1

  公开（公告）日：2000-06-27

  The present invention relates to compounds of formula 1 ##STR1## and to pharmaceutically acceptable salts and solvates thereof, wherein Z, R, R.sup.3 and R.sup.4 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of inhibiting abnormal cell growth, including cancer, in a mammal by administering the compounds of formula 1 to said mammal.

  本发明涉及式1的化合物##STR1##以及其药学上可接受的盐和溶剂化物，其中Z、R、R.sup.3和R.sup.4的定义如本文所述。本发明还涉及含有式1的化合物的药物组合物，以及通过将式1的化合物用于哺乳动物的治疗来抑制异常细胞生长，包括癌症。
• Cyclic ketal beta-secretase inhibitors for the treatment of alzheimer's disease
  申请人：Merck Sharp & Dohme Corp.

  公开号：US07816378B2

  公开（公告）日：2010-10-19

  The present invention is directed to cyclic ketal compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

  本发明涉及公式（I）的环状酯化合物，它们是β-分泌酶酶的抑制剂，并且在治疗β-分泌酶酶参与的疾病，如阿尔茨海默病中有用。本发明还涉及包含这些化合物的制药组合物以及使用这些化合物和组合物治疗β-分泌酶酶参与的这些疾病的方法。
• Cyclic Ketal Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease
  申请人：Nantermet Philippe G.

  公开号：US20090176836A1

  公开（公告）日：2009-07-09

  The present invention is directed to cyclic ketal compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

  本发明涉及公式（I）的环状酯化合物，它们是β-分泌酶酶的抑制剂，可用于治疗β-分泌酶酶参与的疾病，如阿尔茨海默病。本发明还涉及包含这些化合物的制药组合物以及在治疗β-分泌酶酶参与的疾病中使用这些化合物和组合物的用途。
• BENZENE COMPOUND AND MEDICINAL USE THEREOF
  申请人：YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.

  公开号：EP0778263A1

  公开（公告）日：1997-06-11

  A benzene compound of the formula wherein each symbol is as defined in the specification; an optically active isomer or salt thereof, a medicinal composition containing the same, and an immunosuppressant containing the same as the active ingredient. The compound, optically active isomer or salt has an excellent immunosuppressive effect and is useful as an inhibitor for the rejection reaction occurring in organ or bone marrow transplantation, and as a preventive or remedy for articular rheumatism, atopic eczema (dermatitis), Behçet's disease, uveal disease, systemic lupus erythematosus, Sjögren's syndrome, multiple sclerosis, myasthenia gravis, type I diabetes, endocrine ophthalmopathy, primary biliary, cirrhosis, Crohn's disease, glomerulonephritis, sarcoidosis, psoriasis, pemphigus, aplastic anemia, idiopathic thrombocytopenic purpura, allergy, polyarteritis nodosa, progressive systemic sclerosis, mixed connective-tissue disease, aortitis syndrome, polymyositis, dermatomyositis, Wegener's granuloma, ulcerative colitis, active chronic hepatitis, autoimmune hemolytic anemia, Evans' syndrome, bronchial asthma and pollinosis. It is useful also as an antifungal agent and hair growth stimulant.

  式中的苯化合物 其中各符号如说明书中所定义； 其光学活性异构体或盐、含有相同物质的药物组合物，以及含有相同物质作为活性成分的免疫抑制剂。 该化合物、光学活性异构体或盐具有极佳的免疫抑制效果，可作为器官或骨髓移植中发生的排斥反应的抑制剂、可用于预防或治疗关节风湿病、特应性皮炎、白塞氏病、葡萄膜病、系统性红斑狼疮、斯约格伦综合征、多发性硬化症、重症肌无力、I 型糖尿病、内分泌性眼病原发性胆道病、肝硬化、克罗恩病、肾小球肾炎、肉瘤病、银屑病、丘疹性荨麻疹、再生障碍性贫血、特发性血小板减少性紫癜、过敏症、结节性多动脉炎、进行性系统硬化症、混合结缔组织病、大动脉炎综合征、多发性肌炎、皮肌炎、韦格纳肉芽肿、溃疡性结肠炎、活动性慢性肝炎、自身免疫性溶血性贫血、埃文斯综合征、支气管哮喘和花粉症。它还是一种有用的抗真菌剂和生发剂。