sulfamic acid 2-(phenylmethoxy)ethyl ester

• 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: sulfamic acid 2-(phenylmethoxy)ethyl ester
• 英文别名: 2-(Benzyloxy)ethanol sulfamate (ester)；Sulfamic acid 2-(benzyloxy)ethyl ester；2-(Benzyloxy)ethanol sulfamate；2-phenylmethoxyethyl sulfamate
• 化学式: C₉H₁₃NO₄S
• 分子量: 231.273
• InChiKey: AJZOMQLFHYMPFW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  15
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  87
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  2-苄氧基乙醇 、 氨基磺酰氯 在 sulfamic acid 2-(phenylmethoxy)ethyl ester 、 title compound 作用下， 以to give title compound in 54% yield as light-yellow, viscous oil的产率得到sulfamic acid 2-(phenylmethoxy)ethyl ester
  参考文献：
  名称：

  Compounds having one or more aminosulfaonyloxy radicals useful as

  摘要：

  使用已知和新颖化合物治疗慢性关节炎和骨质疏松的方法，这些化合物可以归纳为以下一般公式：（HO）p-A-[-OS（O）2 NR1R2] z，其中A包括广泛的值，包括但不限于芳香族，低烷基，环烷基和碳水化合物，包括蔗糖和果糖；p等于分子中未反应的羟基数，可以为零；z是-OS（O）2 NR1R2基团的数量，始终至少为一；R1和R2从氢，低烷基，羧基等中选择；提供了一种新颖的制备该化合物的方法，其中适当的磺酸芳基酯与含有保护的羧基，氨基或羟基取代基的羟基取代的A基团在含有三级胺碱的无极溶剂中反应。还提供了用于治疗慢性关节炎和骨质疏松的制药组合物。

  公开号：

  US05194446A1
• 作为试剂：
  描述：

  2-苄氧基乙醇 、 氨基磺酰氯 在 sulfamic acid 2-(phenylmethoxy)ethyl ester 、 title compound 作用下， 以to give title compound in 54% yield as light-yellow, viscous oil的产率得到sulfamic acid 2-(phenylmethoxy)ethyl ester
  参考文献：
  名称：

  Sulfamates as antiglaucoma agents

  摘要：

  公式为(HO).sub.p --A--[OSO.sub.2 NR.sup.1 R.sup.2 ].sub.z的磺酰胺酯，其中A为芳氧基烷基，p是烷基部分未反应的羟基数，可以为零，z为连接到烷基部分碳上的--OS(O).sub.2 NR.sup.1 R.sup.2基团数，且始终至少为1；R.sup.1和R.sup.2从氢、低碳基、羧基等中选择，可用于治疗青光眼。

  公开号：

  US05192785A1

文献信息

• Compounds having one or more aminosulfaonyloxy radicals useful as
  申请人：A. H. Robins Company, Incorporated

  公开号：US05194446A1

  公开（公告）日：1993-03-16

  Methods of treating chronic arthritis and osteoporosis which utilize both known and novel compounds which would fall under the general formula: (HO)p--A--[--OS(O).sub.2 NR.sup.1 R.sup.2 ].sub.z wherein A encompasses a wide range of values including but not limited to aryl, loweralkyl, cycloalkyl, and carbohydrates including sucrose and fructose; p is equal to the number of unreacted hydroxy groups contained on the molecule and may be zero; z is the number of --OS(O).sub.2 NR.sup.1 R.sup.2 groups and is always at least one; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, carboxy and the like; a novel process for preparing the compounds is provided wherein an appropriate sulfamic acid aryl ester is reacted with a hydroxy substituted A radical which may or may not contain thereon protected carboxyl, amino or hydroxy substituents, in an aprotic solvent containing a tertiary amine base. Pharmaceutical compositions for the treatment of chronic arthritis and osteoporosis are also provided.

  使用已知和新颖化合物治疗慢性关节炎和骨质疏松的方法，这些化合物可以归纳为以下一般公式：（HO）p-A-[-OS（O）2 NR1R2] z，其中A包括广泛的值，包括但不限于芳香族，低烷基，环烷基和碳水化合物，包括蔗糖和果糖；p等于分子中未反应的羟基数，可以为零；z是-OS（O）2 NR1R2基团的数量，始终至少为一；R1和R2从氢，低烷基，羧基等中选择；提供了一种新颖的制备该化合物的方法，其中适当的磺酸芳基酯与含有保护的羧基，氨基或羟基取代基的羟基取代的A基团在含有三级胺碱的无极溶剂中反应。还提供了用于治疗慢性关节炎和骨质疏松的制药组合物。
• Aryl and aryloxyalkyl sulfamate esters useful as anticonvulsants
  申请人：A. H. Robins Co., Inc.

  公开号：US05025031A1

  公开（公告）日：1991-06-18

  Herein disclosed is a method of treating convulsions with a pharmaceutical composition containing a compound of the formula: (HO).sub.p --A--[OSO.sub.2 NR.sup.1 R.sup.2 ].sub.z where A is an aryl, arylalkyl, or aryloxyalkyl group and is substituted on 1 or more carbon atoms with a sulfamate group (--OSO.sub.2 NR.sup.1 R.sup.2) wherein R.sup.1 and R.sup.2, same or different, are hydrogen or loweralkyl wherein p is 0 or 1 and is the number of untreated hydroxyl groups and z is 1 or 2 and is the number of --OS(O.sub.2)NR.sup.1 R.sup.2 groups. Aryl is selected from phenyl, substituted phenyl, pyridinyl, naphthyl, quinolinyl, and the like. Phenyl substituents are selected from hydrogen, halo, hydroxy, phenyl, phenoxy, benzoyl, loweralkyl, loweralkoxy, carboxy, amino, loweralkylamino, diloweralkylamino, acetamido, cyano, nitro, loweralkoxycarboyl, aminosulfonyl, imidazolyl, triazolyl, and the like. Novel compounds not previously disclosed are also described.

  本文揭示了一种使用含有以下化合物的药物组合物治疗惊厥的方法：(HO).sub.p --A--[OSO.sub.2 NR.sup.1 R.sup.2 ].sub.z其中，A是芳基，芳基烷基或芳氧基烷基基团，并在1个或多个碳原子上用磺酰胺基(--OSO.sub.2 NR.sup.1 R.sup.2)取代，其中R.sup.1和R.sup.2相同或不同，是氢或较低烷基，其中p为0或1，是未处理的羟基数目，z为1或2，是--OS(O.sub.2)NR.sup.1 R.sup.2基团的数目。芳基选自苯基，取代苯基，吡啶基，萘基，喹啉基等。苯基取代基选自氢，卤素，羟基，苯基，苯氧基，苯甲酰基，较低烷基，较低烷氧基，羧基，氨基，较低烷基氨基，二较低烷基氨基，乙酰胺基，氰基，硝基，较低烷氧羰基，氨基磺酰基，咪唑基，三唑基等。还描述了以前未披露的新化合物。
• Compounds having one or more aminosulfonyloxy radicals useful as
  申请人：A. H. Robins Company, Incorporated

  公开号：US05273993A1

  公开（公告）日：1993-12-28

  Methods of treating chronic arthritis and osteoporosis which utilize both known and novel compounds which would fall under the general formula: (HO)p--A--[--OS(O).sub.2 NR.sup.1 R.sup.2 ].sub.z wherein A encompasses a wide range of values including but not limited to aryl, loweralkyl, cycloalkyl, and carbohydrates including sucrose and fructose; p is equal to the number of unreacted hydroxy groups contained on the molecule and may be zero; z is the number of --OS(O).sub.2 NR.sup.1 R.sup.2 groups and is always at least one; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, carboxy and the like; a novel process for preparing the compounds is provided wherein an appropriate sulfamic acid aryl ester is reacted with a hydroxy substituted A radical which may or may not contain thereon protected carboxyl, amino or hydroxy substituents, in an aprotic solvent containing a tertiary amine base. Pharmaceutical compositions for the treatment of chronic arthritis and osteoporosis are also provided.

  本发明涉及治疗慢性关节炎和骨质疏松症的方法，利用已知和新颖化合物，这些化合物可归为以下一般式：（HO）p-A-[-OS（O）.sub.2 NR.sup.1 R.sup.2].sub.z，其中A包括一系列值，包括但不限于芳基，低烷基，环烷基和碳水化合物，包括蔗糖和果糖；p等于分子中未反应的羟基数，可以为零；z是-OS（O）.sub.2 NR.sup.1 R.sup.2基团的数量，始终至少为一；R.sup.1和R.sup.2从氢，低烷基，羧基等中选择；提供了一种新颖的制备该化合物的过程，其中适当的磺酸芳基酯与含有保护羧基，氨基或羟基取代基团的羟基取代A基团在无极溶剂中反应，其中含有三级胺碱。还提供了用于治疗慢性关节炎和骨质疏松症的药物组合物。
• Compounds having one or more aminosulfonyloxy radicals useful as pharmaceuticals
  申请人：A.H. ROBINS COMPANY, INCORPORATED

  公开号：EP0403185A2

  公开（公告）日：1990-12-19

  The invention concerns known and novel compounds which fall under the general formula: wherein A encompasses a wide range of values including but not limited to aryl, loweralkyl, cycloalkyl, and carbohydrates including sucrose and fructose; p is equal to the number of hydroxy groups on A and may be zero; z is the number of -OS(O)2NR1R2 groups and is always at least one; R1 and R2 are selected from hydrogen, loweralkyl, carboxy and the like; which compounds are useful for treating chronic arthritis and osteoporosis. A novel process for preparing the compounds is provided wherein an appropriate sulfamic acid aryl ester is reacted with a a hydroxy substituted A radical which may or may not contain thereon protected carboxyl, amino or hydroxy substituents, in an aprotic solvent containing a tertiary amine base. Pharmaceutical compositions for the treatment of chronic arthritis and osteoporosis are also provided.

  本发明涉及属于通式的已知和新型化合物： 其中，A 的数值范围很广，包括但不限于芳基、低级烷基、环烷基以及包括蔗糖和果糖在内的碳水化合物；p 等于 A 上羟基的数目，可以是零；z 是 -OS(O)2NR1R2 基团的数目，总是至少一个；R1 和 R2 选自氢、低级烷基、羧基等；这些化合物可用于治疗慢性关节炎和骨质疏松症。本发明提供了一种制备这些化合物的新工艺，即在含有叔胺基的钝溶剂中，将适当的氨基磺酸芳基酯与羟基取代的 A 基反应，A 基上可以含有或不含有受保护的羧基、氨基或羟基取代基。此外，还提供了用于治疗慢性关节炎和骨质疏松症的药物组合物。
• US5025031A
  申请人：——

  公开号：US5025031A

  公开（公告）日：1991-06-18