ammonium salt of pravastatin | 151006-11-0

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羟基酸及其衍生物
• 英文名称: ammonium salt of pravastatin
• 英文别名: amine salt of pravastatin；(3R,5R)-7-[(1S,2S,6S,8S,8aR)-6-hydroxy-2-methyl-8-[(2S)-2-methylbutanoyl]oxy-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]-3,5-dihydroxyheptanoic acid;azane
• CAS: 151006-11-0
• 化学式: C₂₃H₃₅O₇*H₄N
• 分子量: 441.565
• InChiKey: ULYXRWWCKJQKDU-IYNICTALSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.48
• 重原子数：
  31
• 可旋转键数：
  11
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.74
• 拓扑面积：
  125
• 氢给体数：
  5
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  ammonium salt of pravastatin 在 硫酸 作用下， 以 乙腈 为溶剂， 反应 0.5h， 生成 普伐他汀类酯
  参考文献：
  名称：

  [EN] LACTONIZATION PROCESS
  [FR] PROCEDE DE LACTONISATION

  摘要：

  本发明揭示了一种制备化合物（II）的过程，包括用硫酸处理化合物（I），其中硫酸以一次性添加，添加量小于化合物（I）的0.8当量；在低于-150摄氏度的温度下；处理时间小于1小时；在水溶性溶剂中进行，最好是乙腈，其中G = 未取代或取代的烷基、芳基或杂环芳基，X = H或金属或胺。

  公开号：

  WO2005012279A1

文献信息

• Pravastatin sodium substantially free of pravastatin lactone and epi-pravastatin, and compositions containing same
  申请人：——

  公开号：US20020082295A1

  公开（公告）日：2002-06-27

  The present invention provides pravastatin sodium substantially free of pravastatin lactone and epiprava, the C-6 epimer of pravastatin. The present invention further provides a novel process for recovering pravastatin sodium from a fermentation broth in such high purity. The process includes the stages of forming an solution of the compound by extraction, obtaining an ammonium salt of pravastatin from the solution, purifying the ammonium salt of the compound and transposing the salt of the compound to pravastatin sodium.

  本发明提供了基本上不含普伐他汀内酯和普伐他汀的盐酸普伐他汀，以及普伐他汀的C-6外消旋体——环氧普伐他汀。本发明还提供了一种从发酵液中以高纯度回收盐酸普伐他汀的新工艺。该工艺包括通过提取形成化合物的溶液，从溶液中获取盐酸普伐他汀的铵盐，纯化该化合物的铵盐，并将该化合物的盐转化为盐酸普伐他汀的阶段。
• Method for the isolation and purification of pravastatin sodium
  申请人：Balkanpharma-Razgrad AD

  公开号：EP1452519A1

  公开（公告）日：2004-09-01

  The invention relates to a method for the isolation and purification of pravastatin sodium, intended for application in the pharmaceutical industry. The application of the method results in pravastatin sodium salt of high yield and purity without recovery and additional purification of intermediate products. After the process the fermentationta broth is alkalized to pH 10.2, centrifuged, the resultant filtrate is extracted with butyl acetate and then reextracted with water. The obtained reextract is treated with sodium hydroxide to concentration of the hydroxide in the reextract of 0.5-4 %, and is again extracted with butyl acetate in the presence of sodium chloride. The precipitation of pravastatin is performed with t-octylamine. The obtained crystalline pravastatin-t-octylamine salt is converted into sodium salt, which is purified and recovered.

  该发明涉及一种用于分离和纯化普伐他汀钠的方法，旨在应用于制药工业。该方法的应用导致高产率和纯度的普伐他汀钠盐，无需回收和进一步纯化中间产物。在该过程中，发酵液被碱化至pH 10.2，离心，所得滤液用丁酸酯萃取，然后再用水重新萃取。获得的再萃取物经过氢氧化钠处理，使再萃取物中氢氧化物的浓度为0.5-4％，然后在氯化钠存在下再次用丁酸酯萃取。普伐他汀的沉淀是用t-辛基胺进行的。获得的结晶普伐他汀-t-辛基胺盐转化为钠盐，经过纯化和回收。
• [EN] PRAVASTATIN SODIUM SUBSTANTIALLY FREE OF PRAVASTATIN LACTONE AND EPI-PRAVASTATIN, AND COMPOSITIONS CONTAINING SAME<br/>[FR] PRAVASTATINE SEL DE SODIUM NE CONTENANT SENSIBLEMENT PAS DE PRAVASTATINE SOUS FORME LACTONE NI D'EPI-PRAVASTATINE, ET COMPOSITIONS CORRESPONDANTES
  申请人：BIOGAL GYOGYSZERGYAR

  公开号：WO2002030415A1

  公开（公告）日：2002-04-18

  The present invention provides pravastatin sodium substantially free of pravastatin lactone and epiprava, the C-6 epimer of pravastatin. The present invention further provides a novel process for recovering pravastatin sodium from a fermentation broth in such high purity. The process includes the stages of forming an solution of the compound by extraction, obtaining an ammonium salt of pravastatin from the solution, purifying the ammonium salt of the compound and transposing the salt of the compound to pravastatin sodium.

  本发明提供了基本不含普伐他汀内酯和普伐他汀的C-6表异构体的普伐他汀钠，同时提供了一种从发酵液中高纯度回收普伐他汀钠的新工艺。该工艺包括以下步骤：通过提取形成化合物的溶液，从溶液中获取普伐他汀的铵盐，纯化化合物的铵盐并将其转化为普伐他汀钠。
• [EN] PROCESS FOR RECOVERING STATIN COMPOUNDS FROM A FERMENTATION BROTH<br/>[FR] PROCEDE PERMETTANT DE RECUPERER DES COMPOSES DE STATINE DANS UN BOUILLON DE FERMENTATION
  申请人：BIOGAL GYOGYSZERGYAR

  公开号：WO2001039768A1

  公开（公告）日：2001-06-07

  A novel process for recovering a compound from a fermentation broth that includes the stages of forming an enriched solution of the compound by extraction, obtaining a salt of the compound from the enriched solution, purifying a salt of the compound and trans-salifying the salt of the compound to a metal salt of the compound is disclosed.

  本发明揭示了一种从发酵液中回收化合物的新工艺，其中包括以下阶段：通过萃取形成化合物的富集溶液，从富集溶液中获取化合物的盐，纯化化合物的盐，并将化合物的盐转化为金属盐。
• Process for recovering statin compounds from a fermentation broth
  申请人：BIOGAL GYOGYSZERGYAR RT.

  公开号：EP1481674A1

  公开（公告）日：2004-12-01

  Process for isolating/purifying pravastatin sodium by solvent extraction, using esters and aqueous solutions.

  利用酯类和水溶液，通过溶剂萃取分离/纯化普伐他汀钠的工艺。