[[(4S,5S)-2,2-二甲基-1,3-二氧戊环-4,5-二基]二(亚甲基)]二[二(4-甲氧基-3,5-二甲基苯基)-膦] | 127797-02-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 中文名称: [[(4S,5S)-2,2-二甲基-1,3-二氧戊环-4,5-二基]二(亚甲基)]二[二(4-甲氧基-3,5-二甲基苯基)-膦]
• 英文名称: (4S,5S)-(-)-4,5-bis-2,2-dimethyl-1,3-dioxolane
• 英文别名: [(4S,5S)-5-[Bis(4-methoxy-3,5-dimethylphenyl)phosphanylmethyl]-2,2-dimethyl-1,3-dioxolan-4-yl]methyl-bis(4-methoxy-3,5-dimethylphenyl)phosphane
• CAS: 127797-02-8
• 化学式: C₄₃H₅₆O₆P₂
• 分子量: 730.862
• InChiKey: SKXXXRFPVHLNLJ-XPSQVAKYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  9
• 重原子数：
  51
• 可旋转键数：
  12
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  55.4
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  4-(3',4'-methylenedioxyphenyl)-3-methoxy-carbonyl-but-3-enoic acid 、 [[(4S,5S)-2,2-二甲基-1,3-二氧戊环-4,5-二基]二(亚甲基)]二[二(4-甲氧基-3,5-二甲基苯基)-膦] 、 chloro (cyclooctadiene) rhodium (I) dimer 生成 (R)-(+)-α-(methylenedioxy-3,4 benzyl)hemisuccinate de methyle
  参考文献：
  名称：

  MORIMOTO, TOSHIAKI;CHIBA, MITSUO;ACHIWA, KAZUO, TETRAHEDRON LETT., 31,(1990) N, C. 261-264

  摘要：

  DOI：
• 作为产物：
  描述：

  (-)-1,4-二-O-甲苯磺酰基-2,3-O-异亚丙基-L-苏糖醇 、 双(3,5二甲基4-甲氧苯基)磷 以65%的产率得到
  参考文献：
  名称：

  MORIMOTO, TOSHIAKI;CHIBA, MITSUO;ACHIWA, KAZUO, CHEM. AND PHARM. BULL., 37,(1989) N1, C. 3161-3163

  摘要：

  DOI：

文献信息

• Process for the preparation of tricyclic amino alcohol derivatives
  申请人：ASAHI KASEI KABUSHIKI KAISHA

  公开号：US20030225289A1

  公开（公告）日：2003-12-04

  A process for the preparation of tricyclic amino alcohol derivatives including 2-[N-[2-(9H-carbazol-2-yloxy)ethyl]]amino-1-[(3-methylsulfonylamino)phenyl]ethanol useful in the treatment of diabetes, obesity, hyperlipidemia and so on; and intermediates as represented by formula (5) or (6) or the like useful in the preparation, wherein R11 is hydrogen or the like; and *1 represents an asymmetric carbon atom. 2-Halo-1-(3-nitrophenyl)ethanone derivatives and 1-(3-nitrophenyl)oxirane derivatives, which are intermediates for the preparation of tricyclic amino alcohol derivatives, are easy of purification, and particularly optically active 1-(3-nitrophenyl)oxirane derivatives are effective in enhancing the optical purities of the final products.

  一种用于制备包括2-[N-[2-(9H-咔唑-2-氧基)乙基]]氨基-1-[3-(甲磺酰氨基)苯基]乙醇在内的三环氨基醇衍生物的方法，该方法在治疗糖尿病、肥胖、高脂血症等方面有用；以及用公式(5)或(6)等表示的中间体，在制备中有用，其中R11是氢等；*1代表一个不对称碳原子。2-卤代-1-(3-硝基苯基)乙酮衍生物和1-(3-硝基苯基)环氧衍生物是用于制备三环氨基醇衍生物的中间体，易于纯化，特别是光学活性的1-(3-硝基苯基)环氧衍生物在提高最终产品的光学纯度方面是有效的。
• METHOD FOR THE PREPARATION OF TRICYCLIC AMINO ALCOHOL DERIVATIVES THROUGH AZIDES
  申请人：Asahi Kasei Kabushiki Kaisha

  公开号：EP1174426A1

  公开（公告）日：2002-01-23

  The present invention is directed to processes for the preparation of a tricyclic amino-alcohol derivative useful for treating and preventing diabetes, obesity, hyperlipidemia and the like, which compound is represented by the formula (1): wherein R1 represents a lower alkyl group or a benzyl group; *1 represents an asymmetric carbon atom; R2 represents a hydrogen atom, a halogen atom or a hydroxyl group; and A represents one of the following groups: wherein X represents NH, O or S; R5 represents a hydrogen atom, a hydroxyl group, an amino group or an acetylamino group; and *2 represents an asymmetric carbon atom when R5 is not a hydrogen atom. The processes of the present invention proceed via azide derivatives and are convenient, practical preparing processes with low cost which comprise a small number of steps with good industrial work efficiency.

  本发明涉及一种用于治疗和预防糖尿病、肥胖、高脂血症等疾病的三环氨基醇衍生物的制备方法，该化合物由以下式子表示（1）： 其中R1代表较低的烷基或苄基；*1代表一个不对称碳原子；R2代表氢原子、卤素原子或羟基；A代表以下其中一种基团： 其中X代表NH、O或S；R5代表氢原子、羟基、氨基或乙酰氨基；*2代表一个不对称碳原子，当R5不是氢原子时。本发明的方法通过叠氮衍生物进行，是方便、实用、成本低廉的制备方法，包括少量步骤且具有良好的工业工作效率。
• PROCESS FOR THE PREPARATION OF TRICYCLIC AMINO ALCOHOL DERIVATIVES
  申请人：Asahi Kasei Kabushiki Kaisha

  公开号：EP1195371A1

  公开（公告）日：2002-04-10

  A process for the preparation of tricyclic amino alcohol derivatives of formula (1) or salts thereof which are useful in the treatment and prevention of diabetes, obesity, hyperlipidemia and so on; and intermediates useful for the process: wherein R1 is lower alkyl group or benzyl; *1 represents an asymmetric carbon atom; R2 is hydrogen, halogen, or hydroxyl; and A is one of the following groups: (wherein X is NH, O or S; R6 is hydrogen, hydroxyl, amino, or acetylamino; and *2 represents an asymmetric carbon atom when R6 is not hydrogen)

  一种用于制备式（1）的三环氨基醇衍生物或其盐的方法，该方法有助于治疗和预防糖尿病、肥胖、高脂血症等疾病；以及用于该方法的中间体：其中R1是较低的烷基或苄基；*1代表一个不对称碳原子；R2是氢、卤素或羟基；A是以下组之一：（其中X是NH、O或S；R6是氢、羟基、氨基或乙酰氨基；当R6不是氢时，*2代表一个不对称碳原子）
• PROCESSES FOR THE PREPARATION OF TRICYCLIC AMINO ALCOHOL DERIVATIVES
  申请人：Asahi Kasei Kabushiki Kaisha

  公开号：EP1209150A1

  公开（公告）日：2002-05-29

  A process for the preparation of tricyclic amino alcohol derivatives including 2-[N-[2-(9H-carbazol-2-yloxy)ethyl]]amino-1-[(3-methylsulfonylamino)phenyl]ethanol useful in the treatment of diabetes, obesity, hyperlipidemia and so on; and intermediates as represented by formula (5) or (6) or the like useful in the preparation, wherein R11 is hydrogen or the like; and *1 represents an asymmetric carbon atom. 2-Halo-1-(3-nitrophenyl)ethanone derivatives and 1-(3-nitrophenyl)oxirane derivatives, which are intermediates for the preparation of tricyclic amino alcohol derivatives, are easy of purification, and particularly optically active 1-(3-nitrophenyl)oxirane derivatives are effective in enhancing the optical purities of the final products.

  一种制备三环氨基醇衍生物的工艺，包括用于治疗糖尿病、肥胖症、高脂血症等的2-[N-[2-(9H-咔唑-2-氧基)乙基]]氨基-1-[(3-甲磺酰氨基)苯基]乙醇；以及用于制备的式(5)或式(6)或类似物所代表的中间体，其中R11为氢或类似物；*1代表不对称碳原子。2-Halo-1-(3-nitrophenyl)ethanone 衍生物和 1-(3-硝基苯基)环氧乙烷衍生物是制备三环氨基醇衍生物的中间体，易于纯化，特别是具有光学活性的 1-(3-硝基苯基)环氧乙烷衍生物可有效提高最终产品的光学纯度。
• US6696573B1
  申请人：——

  公开号：US6696573B1

  公开（公告）日：2004-02-24