(1S)-amino-(2R)-indanol | 1315054-53-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 茚满类
• 英文名称: (1S)-amino-(2R)-indanol
• 英文别名: 1S-amino-2R-indanol；cis-(1S)-amino-(2r)-indanol；(1S)-1-amino-2,3-dihydroinden-1-ol
• CAS: 1315054-53-5
• 化学式: C₉H₁₁NO
• 分子量: 149.192
• InChiKey: HDXFCPZKMFTOLH-VIFPVBQESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  11
• 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：
  46.2
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  cis-(1S,2R)-indanediol 在 氢氧化钾 、 硫酸 作用下， 以 水 、 乙腈 为溶剂， 生成 (1S)-amino-(2R)-indanol
  参考文献：
  名称：

  Process for preparing

  摘要：

  使用手性氢化的改进过程，用于高产率合成4-保护基-(S)-哌嗪-2-叔丁基-羧酰胺，这是HIV蛋白酶抑制剂的中间体。

  公开号：

  US05723615A1

文献信息

• Process to make HIV protease inhibitor from
  申请人：Merck & Co., Inc.

  公开号：US05618937A1

  公开（公告）日：1997-04-08

  A process for making a clinically efficacious HIV protease inhibitor eliminates one step in its synthesis, by an alternative convergent synthesis using 2(S)-4-picolyl-2-piperazine-t-butylcarboxamide as an intermediate.

  一种制备临床有效的HIV蛋白酶抑制剂的方法通过使用2(S)-4-吡啶基-2-哌嗪-叔丁基甲酰胺作为中间体，采用另一种收敛合成方法，省略了合成过程中的一步。
• Chiral bisphosphines
  申请人：Merck & Co., Inc.

  公开号：US05874629A1

  公开（公告）日：1999-02-23

  New chiral biphosphines, e.g., ##STR1## are useful as key components in catalysts for asymmetric reactions, providing desirably high enantiomeric excess (ee).

  新的手性双膦化合物，例如##STR1##，在不对称反应的催化剂中作为关键组分非常有用，能够提供理想高的对映体过量（ee）。
• Chemically modified mutant serine hydrolases show improved catalytic activity and chiral selectivity
  申请人：Jones Bryan John

  公开号：US20050282248A1

  公开（公告）日：2005-12-22

  This invention provides novel chemically modified mutant serine hydrolases that catalyze a transamidation and/or a transpeptidation and/or a transesterification reaction. The modified serine hydrolases have one or more amino acid residues in a subsite replaced with a cysteine, wherein the cysteine is modified by replacing the thiol hydrogen in the cysteine with a substituent group providing a thiol side chain comprising a moiety selected from the group consisting of a polar aromatic substituent, an alkyl amino group with a positive charge, and a glycoside. In particularly preferred embodiments, the substitutents include an oxazolidinone, a C 1 to C 15 alkyl amino group with a positive charge, or a glycoside.

  该发明提供了一种新型的化学修饰突变丝氨酸水解酶，其催化转酰胺化和/或转肽化和/或酯交换反应。改性的丝氨酸水解酶具有一个或多个氨基酸残基在一个亚位点上被取代为半胱氨酸，其中半胱氨酸通过用提供来自一组成员的基团的硫醇侧链替换半胱氨酸中的硫氢原子而进行修饰，所述基团包括极性芳香基团、带有正电荷的烷基氨基团和糖苷。在特别优选的实施方式中，取代基包括噁唑啉酮、具有正电荷的C1到C15烷基氨基团或糖苷。
• Antidiabetic bicyclic compounds
  申请人：Ge Min

  公开号：US20070265332A1

  公开（公告）日：2007-11-15

  Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

  含有环丙基羧酸或羧酸衍生物（如酰胺）的三环化合物与融合到双环环上的G蛋白偶联受体40（GPR40）是激动剂，并且可用作治疗化合物，特别是在治疗2型糖尿病方面，以及与该疾病常相关的病症，包括肥胖和脂质紊乱，如混合性或糖尿病性脂质代谢异常、高血脂、高胆固醇血症和高甘油三酯血症。
• 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。