(4R-cis)-6-(2-aminoethyl)-2,2-dimethyl-N,N-bis(phenylmethyl)-1,3-dioxane-4-acetamide | 156051-86-4

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (4R-cis)-6-(2-aminoethyl)-2,2-dimethyl-N,N-bis(phenylmethyl)-1,3-dioxane-4-acetamide
• 英文别名: 2-[(4R,6R)-6-(2-aminoethyl)-2,2-dimethyl-1,3-dioxan-4-yl]-N,N-dibenzylacetamide
• CAS: 156051-86-4
• 化学式: C₂₄H₃₂N₂O₃
• 分子量: 396.53
• InChiKey: GXDSSHCTOFRRHH-FGZHOGPDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  29
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  64.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  (4R-cis)-6-(cyanomethyl)-2,2-dimethyl-N,N-bis(phenylmethyl)-1,3-dioxane-4-acetamide 、 氨 、 氢气 在 镍 作用下， 以 甲醇 为溶剂， 以to give 9.4 g of (4R-cis)-6-(2-aminoethyl)-2,2-dimethyl-N,N-bis(phenylmethyl) -1,3-dioxane-4-acetamide as an oil的产率得到(4R-cis)-6-(2-aminoethyl)-2,2-dimethyl-N,N-bis(phenylmethyl)-1,3-dioxane-4-acetamide
  参考文献：
  名称：

  Process for trans-6[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one

  摘要：

  本发明提供了一种改进的方法，通过一种新的合成方法制备转-6-[2-(取代吡咯-1-基)烷基]吡喃-2-酮，其中α-金属化N，N-二取代乙酰胺在七个步骤中转化为所需的产物，具体地，提供了一种制备(2R-转)-5-(4-氟苯基)-2-(1-甲基乙基)-N，4-二苯基-1-[2-(四氢-4-羟基-6-氧代-2H-吡喃-2-基)乙基]-1H-吡咯-3-羧酰胺以及用于该过程和前药的其他有价值的中间体，这些前药被生物转化为降血脂和降胆固醇药物和相应的制药组合物。

  公开号：

  US05489690A1

文献信息

• PROCESSES FOR PREPARING AMINE SALTS OF SILDENAFIL-ANALOGUES AND USE THEREOF
  申请人：Chen Ing-Jun

  公开号：US20120108604A1

  公开（公告）日：2012-05-03

  A series of amine salts including a structure of formula (I) and formula (III) have provided. In formula I or formula (III), R 1 , R a and RX are as defined in the specification. The amine complex salts disclosed in the present invention are characterized in a pro-drug active form and various pharmaceutical function.

  提供了一系列包括公式(I)和公式(III)结构的胺盐。在公式I或公式(III)中，R1、Ra和RX如说明书中所定义。本发明公开的胺络合盐具有前药活性形式和多种药理功能。
• Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one
  申请人：Warner-Lambert Company

  公开号：US05397792A1

  公开（公告）日：1995-03-14

  An improved process for the preparation of trans-6-[2-(substituted-pyrrole-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where .alpha.-metalated N,N-disubstituted acetamide is converted in seven operations to the desired products, and specifically, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl) -N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyr role-3-carboxamide, as well as other valuable intermediates used in the processes and prodrugs which are bioconverted to hypolipidemic and hypocholesterolemic agents and pharmaceutical compositions of the same.

  本发明描述了一种改进的方法，通过一种新的合成方法制备转-6-[2-(取代吡咯-1-基)烷基]吡喃-2-酮，其中α-金属化N，N-二取代乙酰胺经过七次操作转化为所需产品，具体地，本发明还涉及制备(2R-转)-5-(4-氟苯基)-2-(1-甲基乙基)-N,4-二苯基-1-[2-(四氢-4-羟基-6-氧代-2H-吡喃-2-基)乙基]-1H-吡咯-3-羧酰胺以及用于该过程和前药的其他有价值的中间体，这些前药可被生物转化为降脂和降胆固醇剂和相应的药物组成。
• Process for trans-6-(2-(substituted-pyrrol-1-yl)alkyl)pyran-2-one
  申请人：Warner-Lambert Company

  公开号：US05489691A1

  公开（公告）日：1996-02-06

  An improved process for the preparation of trans-6-[2-(substituted-pyrrole-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where .alpha.-metalated N,N-disubstituted acetamide is converted in seven operations to the desired products, and specifically, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahy dro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide, as well as other valuable intermediates used in the processes and prodrugs which are bioconverted to hypolipidemic and hypocholesterolemic agents and pharmaceutical compositions of the same.

  本文描述了一种改进的方法，通过一种新的合成方法制备转-6-[2-(取代吡咯-1-基)烷基]吡喃-2-酮，其中α-金属化的N,N-二取代乙酰胺经过七个步骤转化为所需的产物，具体地，一种制备(2R-转)-5-(4-氟苯基)-2-(1-甲基乙基)-N,4-二苯基-1-[2-(四氢-4-羟基-6-氧代-2H-吡喃-2-基)乙基]-1H-吡咯-3-羧酰胺，以及用于该过程和生物转化为降血脂和降胆固醇药剂的其他有价值的中间体和前药的方法和制药组合物。
• Processes for preparing calcium salt forms of statins
  申请人：Niddam-Hildesheim Valerie

  公开号：US20050197501A1

  公开（公告）日：2005-09-08

  Processes for preparing a calcium salt of a statin from an ester derivative or protected ester derivative of the statin by using calcium hydroxide are provided. The ester or protected ester derivative is contacted with calcium hydroxide to obtain the calcium salt. Preferred statins are rosuvastatin, pitavastatin and atorvastatin, simvastatin and lovastatin. In processes beginning with a protected statin ester derivative, the protecting group is hydrolyzed during salt formation by contact with calcium hydroxide, or is contacted with an acid catalyst followed by contact with calcium hydroxide.

  本发明提供了一种使用氢氧化钙从他汀的酯衍生物或保护酯衍生物制备钙盐的过程。将酯或保护酯衍生物与氢氧化钙接触，以获得钙盐。首选他汀是罗伊司他、匹伐他汀和阿托伐他汀、辛伐他汀和洛伐他汀。在以保护的他汀酯衍生物开始的过程中，保护基在与氢氧化钙接触时水解，在盐形成过程中，或与酸催化剂接触后再与氢氧化钙接触。
• Process for trans-6- 2-(substituted-pyrrol-1-yl)alkyl!pyran-2-one
  申请人：Warner-Lambert Company

  公开号：US05510488A1

  公开（公告）日：1996-04-23

  An improved process for the preparation of trans-6- 2-(substituted-pyrrole-1-yl)alkyl!pyran-2-ones by a novel synthesis is described where .alpha.-metalated N,N-disubstituted acetamide is converted in seven operations to the desired products, and specifically, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N, 4-diphenyl-1- 2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl!-1H-pyrrol e-3-carboxamide, as well as other valuable intermediates used in the processes and prodrugs which are bioconverted to hypolipidemic and hypocholesterolemic agents and pharmaceutical compositions of the same.

  本文介绍了一种改进的制备转-6-2-(取代吡咯-1-基)烷基!吡喃-2-酮的新型合成方法，其中α-金属化N，N-二取代乙酰胺经过七步反应转化为所需的产物，具体地，本文介绍了一种制备(2R-转)-5-(4-氟苯基)-2-(1-甲基乙基)-N，4-二苯基-1- 2-(四氢-4-羟基-6-氧代-2H-吡喃-2-基)乙基!-1H-吡咯烷-3-羧酰胺以及用于该过程和前药的其他有价值的中间体，这些前药可生物转化为降脂和降胆固醇剂和同类的制药组合物。