(2S,4S)-6-氟-2，3-二氢-2’,5’-二氧螺(4H-1-苯并吡喃-4,4’-咪唑烷)-2-羧酸正丙酯 | 136087-83-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑烷类
• 中文名称: (2S,4S)-6-氟-2，3-二氢-2’,5’-二氧螺(4H-1-苯并吡喃-4,4’-咪唑烷)-2-羧酸正丙酯
• 中文别名: (2S,4S)-6-氟-2.3-二氢-2`,5`-二氧螺(4H-1-苯并吡喃-4,4`-咪唑烷)-2-羧酸正丙酯
• 英文名称: (2S,4S)-6-Fluoro-2',5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxylic acid 2-propyl ester
• 英文别名: (2S,4S)-6-fluoro-2,3-dihydro-2',5'-dioxospiro<4H-1-benzopyran-4,4'-imidazolidine>-2-carboxylic acid n-propyl ester；(2S,4S)-6-fluoro-2',5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxylic acid n-propyl ester；(2S,4S)-6-fluoro-2,3-dihydro-2',5'-dioxospiro(4H-1-benzopyran-4,4'-imidazolidine)-2-carboxylic acid n-propyl ester；propyl (2S,4S)-6-fluoro-2',5'-dioxospiro[2,3-dihydrochromene-4,4'-imidazolidine]-2-carboxylate
• CAS: 136087-83-7
• 化学式: C₁₅H₁₅FN₂O₅
• 分子量: 322.293
• InChiKey: KXSOZSJFADAYID-NHYWBVRUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  23
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  93.7
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  (2S,4S)-6-氟-2，3-二氢-2’,5’-二氧螺(4H-1-苯并吡喃-4,4’-咪唑烷)-2-羧酸正丙酯 在 氨 作用下， 以 甲醇 为溶剂， 反应 4.0h， 以92.2%的产率得到非达司他
  参考文献：
  名称：

  Yamaguchi; Miura; Usui, Arzneimittel-Forschung/Drug Research, 1994, vol. 44, # 3, p. 344 - 348

  摘要：

  DOI：
• 作为产物：
  描述：

  （2S）-6-氟-3，4-二氢-4-氧代-2H-1-苯并吡喃-2-甲酸 在 硫酸 碳酸氢铵 作用下， 以 水 、 苯 为溶剂， 反应 6.0h， 生成 (2S,4S)-6-氟-2，3-二氢-2’,5’-二氧螺(4H-1-苯并吡喃-4,4’-咪唑烷)-2-羧酸正丙酯
  参考文献：
  名称：

  Yamaguchi; Miura; Usui, Arzneimittel-Forschung/Drug Research, 1994, vol. 44, # 3, p. 344 - 348

  摘要：

  DOI：

文献信息

• Hydantoin derivatives for treating complications of diabetes and
  申请人：Sanwa Kagaku Kenkyusho Co., Ltd.

  公开号：US05164391A1

  公开（公告）日：1992-11-17

  The invention relates to a hydantoin derivative, salt thereof, process for the preparation thereof, and medicine containing the derivative. The derivative is represented by the formula ##STR1## wherein M is --CONH--NHR.sup.1 group, --CONH--OR.sup.2 group, ##STR2## in which R.sup.1 is hydrogen atom, an alkyl group, an alkenyl group, a phenyl radical, a substituted phenyl group, a naphthyl radical, a substituted naphthyl group, a pyridyl radical, a furyl radical or a thienyl radical, R.sup.2 is a hydrogen atom, an alkyl group, a phenyl radical or a substituted phenyl group, R.sup.3 and R.sup.4 are the same or different independently, each being a phenyl radical, or an aralkyl group, or R.sup.3 may form a substituted or non-substituted C.sub.5-6 saturated heterocyclic ring together with R.sup.4 and a possible nitrogen or oxygen atom, R.sup.5 forms a substituted or non-substituted saturated heterocyclic ring together with R.sup.6 and a possible nitrogen or oxygen atom, R.sup.7 is a nitroxy radical or a heteroaryl group, .sub.m and .sub.n are an integer of 2 to 5, Q is a hydrogen atom or ##STR3## in which R.sup.8 and R.sup.9 are the same or different independently, each being a substituted or non-substituted alkyl group, or R.sup.8 may form a substituted or non-substituted C.sub.5-6 saturated heterocyclic ring together with R.sup.9 and a possible nitrogen or oxygen atom, .sub.r is an integer of 2 to 5, T and X are the same or different independently, each being a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or an alkylmercapto group, and Z is an oxygen or sulfur atom. The derivatives and salts thereof are useful for the treatment of complications of diabetes and circulatory diseases.

  该发明涉及一种咪唑烷酮衍生物及其盐，其制备方法以及含有该衍生物的药物。该衍生物由以下结构表示：其中 M 是--CONH--NHR.sup.1基团，--CONH--OR.sup.2基团，R.sup.1 是氢原子，烷基，烯基，苯基，取代苯基，萘基，取代萘基，吡啶基，呋喃基或噻吩基，R.sup.2 是氢原子，烷基，苯基或取代苯基，R.sup.3 和 R.sup.4 独立相同或不同，各自是苯基或芳基烷基，或 R.sup.3 可与 R.sup.4 一起形成取代或非取代的C.sub.5-6饱和杂环环，其中可能包括一个氮原子或氧原子，R.sup.5 与 R.sup.6 一起形成取代或非取代的饱和杂环环，其中可能包括一个氮原子或氧原子，R.sup.7 是亚硝基基团或杂芳基团，m 和 n 是2到5的整数，Q 是氢原子或##STR3##，其中 R.sup.8 和 R.sup.9 独立相同或不同，各自是取代或非取代的烷基，或 R.sup.8 可与 R.sup.9 一起形成取代或非取代的C.sub.5-6饱和杂环环，其中可能包括一个氮原子或氧原子，r 是2到5的整数，T 和 X 独立相同或不同，各自是氢原子，卤原子，烷基，烷氧基或烷巯基，Z 是氧原子或硫原子。这些衍生物及其盐对于治疗糖尿病和循环疾病的并发症是有用的。
• Hydantoin derivatives for treating complications of diabetes and circulatory diseases
  申请人：SANWA KAGAKU KENKYUSHO CO., LTD.

  公开号：EP0418834A1

  公开（公告）日：1991-03-27

  The invention relates to a hydantoin derivative, salt thereof, process for the preparation thereof, and medicine containing the derivative. The derivative is represented by the formula wherein M is -CONH-NHR' group, -CONH-OR2 group, or -CONH(CH2)nR7 group, in which R1 is hydrogen atom, an alkyl group, an alkenyl group, a phenyl radical, a substituted phenyl group, a naphtyl radical, a substituted naphtyl group, a pyridyl radical, a furyl radical or a thienyl radical, R2 is a hydrogen atom, an alkyl group, a phenyl radical or a substituted phenyl group, R3 and R4 are same or different independently, each being a hydrogen atom, an alkyl group, a phenyl radical, a substituted phenyl group or an aralkyl group, or R3 may form a substituted or non-substituted C5-6 saturated heterocyclic ring together with R4 and a possible nitrogen or oxygen atom, R5 forms a substituted or non-substituted saturated heterocyclic ring together with R6 and a possible nitrogen or oxygen atom, R7 is a nitroxy radical or a heteroaryl group, m and n are an integer of 2 to 5, Q is a hydrogen atom or in which R8 and R9 are same or different independently, each being a substituted or non-substituted alkyl group, or R8 may form a substituted or non-substituted Cs-6 saturated heterocyclic ring together with R9 and a possible nitrogen or oxygen atom, is an integer of 2 to 5, T and X are same or different independently, each being a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or an alkylmercapto group, and Z is an oxygen or sulfur atom. The derivatives and salts thereof are useful for the treatment of complications of diabetes and circulatory diseases.

  本发明涉及一种海因衍生物、其盐、其制备工艺以及含有该衍生物的药物。该衍生物由式表示 其中 M 为-CONH-NHR'基团、-CONH-OR2 基团、 或-CONH(CH2)nR7 基团，其中 R1 是氢原子、烷基、烯基、苯基、取代苯基、萘基、取代萘基、吡啶基、呋喃基或噻吩基，R2 是氢原子、烷基、苯基或取代苯基，R3 和 R4 独立地相同或不同，各自是氢原子、烷基、苯基或取代苯基、或 R3 可与 R4 和一个可能的氮原子或氧原子一起形成一个取代或非取代的 C5-6 饱和杂环，R5 与 R6 和一个可能的氮原子或氧原子一起形成一个取代或非取代的饱和杂环，R7 是硝酸基或杂芳基，m 和 n 是 2 至 5 的整数，Q 是氢原子，或 其中 R8 和 R9 独立地相同或不同，各自为取代或非取代的烷基，或 R8 可与 R9 和可能的氮原子或氧原子一起形成取代或非取代的 Cs-6 饱和杂环，为 2 至 5 的整数，T 和 X 独立地相同或不同，各自为氢原子、卤素原子、烷基、烷氧基或烷基巯基，Z 为氧原子或硫原子。这些衍生物及其盐类可用于治疗糖尿病并发症和循环系统疾病。
• Hydantoin derivatives, salts thereof and maillard reaction inhibitors comprising the same
  申请人：SANWA KAGAKU KENKYUSHO CO., LTD.

  公开号：EP0595183B1

  公开（公告）日：1999-08-25
• US5164391A
  申请人：——

  公开号：US5164391A

  公开（公告）日：1992-11-17
• Yamaguchi; Miura; Usui, Arzneimittel-Forschung/Drug Research, 1994, vol. 44, # 3, p. 344 - 348
  作者：Yamaguchi、Miura、Usui、Unno、Matsumoto、Fukushima、Mizuno、Kondo、Baba、Kurono

  DOI：——

  日期：——