4-Aminochroman-3-ol | 454679-90-4

• 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: 4-Aminochroman-3-ol
• 英文别名: 4-amino-3,4-dihydro-2H-chromen-3-ol
• CAS: 454679-90-4
• 化学式: C₉H₁₁NO₂
• 分子量: 165.192
• InChiKey: JVPRWKWUBCZNJO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  55.5
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2,3-二氢苯并吡喃-4-酮 在 吡啶 、 盐酸 、 氢氧化钾 、 硼烷四氢呋喃络合物 、 碘苯二乙酸 作用下， 以 四氢呋喃 为溶剂， 反应 50.0h， 生成 4-Aminochroman-3-ol
  参考文献：
  名称：

  立体选择性还原α-羟基肟醚：制备顺式1,2-氨基醇的简便方法

  摘要：

  用硼烷还原环状α-羟基酮肟可提供极好的，高产率的区域和立体选择路线，生成-1,2-氨基醇。

  DOI：

  10.1016/s0040-4039(00)74864-7

文献信息

• Cinnamide compound
  申请人：Kimura Teiji

  公开号：US20060004013A1

  公开（公告）日：2006-01-05

  The present invention relates to a compound represented by Formula (I): (wherein Ar 1 represents an imidazolyl group which may be substituted with 1 to 3 substituents; Ar 2 represents a pyridinyl group, a pyrimidinyl group, or a phenyl group which may be substituted with 1 to 3 substituents; X 1 represents (1) —C≡C— or (2) a double bond etc. which may be substituted; R 1 and R 2 represent, for example, a C1-6 alkyl group or C3-8 cycloalkyl group which may be substituted) or a pharmacologically acceptable salt thereof and to the use thereof as pharmaceutical agents. The object of the present invention is to find a therapeutic or preventive agent for diseases caused by Aβ. According to the present invention, a therapeutic or preventive agents for diseases caused by Aβ can be provided.

  本发明涉及一种由式（I）表示的化合物：（其中Ar1代表可以被1到3个取代基取代的咪唑基团；Ar2代表可以被1到3个取代基取代的吡啶基团、嘧啶基团或苯基；X1代表（1）-C≡C-或（2）可以被取代的双键等；R1和R2代表，例如，可以被取代的C1-6烷基或C3-8环烷基等）或其药理学上可接受的盐，并且用作药物剂。本发明的目的是寻找一种治疗或预防由Aβ引起的疾病的药剂。根据本发明，可以提供治疗或预防由Aβ引起的疾病的药剂。
• Process for preparing acetonides
  申请人：——

  公开号：US20020132837A1

  公开（公告）日：2002-09-19

  Acetonides are obtained in a one-step reaction of a carboxylic acid halide, a 1,2-aminoalcohol, and 2-alkoxypropene or 2,2-dialkoxypropane in an ether solvent and in the presence of an inorganic base. Acetonides are also obtained in a two-step reaction scheme in which an acid halide and 1,2-aminoalcohol are reacted in an ether solvent in the presence of LiOH to form a hydroxyamide, which is then reacted with 2-alkoxypropene or 2,2-dialkoxypropane in the presence of acid to form the acetonide. The acetonides resulting from the one-step and two-step protocols can be further reacted with an allylating agent such as an allyl halide in the presence of a strong base to provide the corresponding allyl acetonide. The acetonides and allyl acetonides can serve as intermediates in the production of certain HIV protease inhibitors which are useful for treating HIV infection and AIDS.

  Acetonides是通过在醚溶剂中，在无机碱的存在下，将羧酸卤、1,2-氨基醇和2-烷氧基丙烯或2,2-二烷氧基丙烷进行一步反应而获得的。Acetonides也可以通过两步反应方案获得，其中酸卤和1,2-氨基醇在醚溶剂中在LiOH的存在下反应以形成羟基酰胺，然后在酸的存在下与2-烷氧基丙烯或2,2-二烷氧基丙烷反应以形成缩醛。通过一步和两步方案得到的缩醛可以进一步与烯丙基卤等烯丙基化试剂在强碱的存在下反应，从而得到相应的烯丙基缩醛。这些缩醛和烯丙基缩醛可以作为某些用于治疗HIV感染和艾滋病的HIV蛋白酶抑制剂的生产中间体。
• Process for preparing cis- aminochromanols
  申请人：——

  公开号：US20010056193A1

  公开（公告）日：2001-12-27

  cis-aminochromanols are obtained in high yield and with high selectivity over their trans counterparts by hydrogenating the corresponding oximes in the presence of a catalyst and an acid selected from HBr, HCl, and organic sulfonic acid. The cis-aminochromanols can be employed as intermediates in the production of HIV protease inhibitors which are useful for treating HIV infection and AIDS.

  在催化剂和选自HBr、HCl和有机磺酸的酸存在下，通过对应的肟的加氢反应高产率高选择性地得到顺式-氨基色满醇，而不是其反式对应物。顺式-氨基色满醇可用作HIV蛋白酶抑制剂的中间体，这些抑制剂对治疗HIV感染和艾滋病非常有用。
• Process for preparing hydroxychomanones and CIS-aminochromanols
  申请人：——

  公开号：US20020095047A1

  公开（公告）日：2002-07-18

  Enantiomerically enriched hydroxychromanones are obtained by the AlCl 3 -catalyzed intramolecular Friedel-Crafts acylation of the corresponding 3-phenoxy-2-alkylcarbonyloxy-propionic acid followed by cleavage of the carboxylate in the presence of an alkali metal peroxide or hydroperoxide. Enantiomerically enriched cis-aminochromanols can then be prepared by treating the hydroxychromanones with a hydroxylamine and hydrogenating the resulting oxime. The cis-aminochromanols can be employed as intermediates in the production of HIV protease inhibitors which are useful for treating HIV infection and AIDS.

  手性富集的羟基色酮可以通过AlCl3催化的相应3-苯氧基-2-烷基羧酰氧基丙酸的分子内Friedel-Crafts酰化反应获得，然后在碱金属过氧化物或过氧化氢存在下断开羧酸酯键。然后，通过将羟基色酮与羟肟反应并加氢得到手性富集的顺式氨基色醇。顺式氨基色醇可用作HIV蛋白酶抑制剂的中间体，这些抑制剂对治疗HIV感染和艾滋病有用。
• [EN] HIV PROTEASE INHIBITORS SUPPORTED ON CATION EXCHANGE RESINS FOR ORAL ADMINISTRATION<br/>[FR] INHIBITEURS DE LA PROTEASE VIH RETENUS SUR DES SUPPORTS EN RESINES D'ECHANGE DE CATIONS DESTINES A L'ADMINISTRATION PAR VOIE ORALE
  申请人：MERCK & CO INC

  公开号：WO2002067683A1

  公开（公告）日：2002-09-06

  γ-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds useful for inhibiting HIV protease and HIV replication and useful in the prevention or treatment of infection by HIV and the treatment of AIDS are complexed with cation exchange resins for oral administration.

  γ-羟基-2-（氟烷基氨基甲酰基）-1-哌嗪戊酰胺化合物可用于抑制HIV蛋白酶和HIV复制，并用于预防或治疗HIV感染和治疗艾滋病，与阳离子交换树脂形成复合物，以进行口服给药。