(2R)-2-methyl-2-dimethoxymethyl-2H-1-benzopyran | 335382-03-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: (2R)-2-methyl-2-dimethoxymethyl-2H-1-benzopyran
• 英文别名: (2R)-2-(dimethoxymethyl)-2-methylchromene
• CAS: 335382-03-1
• 化学式: C₁₃H₁₆O₃
• 分子量: 220.268
• InChiKey: JXWOBHOYWNHORP-CYBMUJFWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  27.7
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (2R)-2-methyl-2-dimethoxymethyl-2H-1-benzopyran 在 N-溴代丁二酰亚胺(NBS) 、 水 、 sodium hydroxide 作用下， 以 1,4-二氧六环 、 水 为溶剂， 反应 0.9h， 以83%的产率得到(2R)-2-methyl-2-dimethoxymethyl-3,4-epoxy-3,4-dihydro-2H-1-benzopyran
  参考文献：
  名称：

  BENZOPYRANYL GUANIDINE DERIVATIVES, PROCESS FOR PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

  摘要：

  公开号：

  EP1228058B1

文献信息

• [EN] BENZOPYRANYL GUANIDINE DERIVATIVES, PROCESS FOR PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM<br/>[FR] DERIVES DE BENZOPYRANYLE GUANIDINE, LEUR PROCEDE DE PREPARATION ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT
  申请人：KOREA RES INST CHEM TECH

  公开号：WO2001029023A1

  公开（公告）日：2001-04-26

  The present invention relates to novel benzopyranyl guanidine derivatives of formula (1), wherein R1, R2, R3, R4, R5, R6, n and * are each defined in specification, process for preparation thereof and pharmaceutical use of the benzopyranyl guanidine derivatives. The benzopyranyl guanidine derivatives of the present invention can be used for protecting heart, neuronal cell or brain damage, preserving organs, and also the benzopyranyl guanidine derivatives are pharmacologically useful for inhibiting NO generation, and for suppressing lipid peroxidation, angiogenesis or restenosis.

  本发明涉及一种新型苯并吡啶基胍衍生物，其化学式为（1），其中R1，R2，R3，R4，R5，R6，n和*在规范中各自定义，制备过程以及苯并吡啶基胍衍生物的药用。本发明的苯并吡啶基胍衍生物可用于保护心脏、神经细胞或脑损伤，保护器官，也可用于药理学上抑制NO的生成，抑制脂质过氧化，抑制血管生成或再狭窄。
• EP1228058A4
  申请人：——

  公开号：EP1228058A4

  公开（公告）日：2003-02-12
• BENZOPYRANYL HETEROCYCLE DERIVATIVES, PROCESS FOR PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
  申请人：Dongbu Hitek Co., Ltd.

  公开号：EP1330454B1

  公开（公告）日：2010-05-19
• Topical Formulations Comprising Ion Channel Modulators
  申请人：Blum Steven

  公开号：US20110020453A1

  公开（公告）日：2011-01-27

  Disclosed herein are pharmaceutical formulations comprising particles of formula 1: wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , n and * are each defined in specification. Also disclosed are methods of decreasing intraocular pressure comprising topically applying a benzopyranyl guanidine derivative of formula 1 to an eye.
• TOPICAL OPHTHALMIC PHARMACEUTICAL FORMULATION OF (2S,3S,4R)-N''-CYANO-N-(6-AMINO-3,4-DIHYDRO-3-HYDROXY-2-METHYL-2-DIMETHOXYMETHYL-2H-BENZOPYRAN-4-YL)-N'-BENZYLGUANIDINE
  申请人：Blum Steven

  公开号：US20110070310A1

  公开（公告）日：2011-03-24

  A topical ophthalmic pharmaceutical formulation may include particles of the compound (2S,3S,4R)—N″-cyano-N-(6-amino-3,4-dihydro-3-hydroxy-2-methyl-2-dimethoxymethyl-2H-benzopyran-4-yl)-N′-benzylguanidine suspended in a solution comprising monobasic sodium phosphate monohydrate, disodium phosphate heptahydrate, edetate disodium, benzalkonium chloride, sodium chloride, polysorbate 80, and water. A method of treating glaucoma may include topically applying to the eye of a patient in need thereof a therapeutically effective amount of this formulation.