7-(2-Cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl)-3,5-dihydroxyhept-6-enoic acid | 121659-03-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 7-(2-Cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl)-3,5-dihydroxyhept-6-enoic acid
• 英文别名: 7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxyhept-6-enoic acid
• CAS: 121659-03-8
• 化学式: C₂₅H₂₄FNO₄
• 分子量: 421.5
• InChiKey: VGYFMXBACGZSIL-UHFFFAOYSA-N

物化性质

• 沸点：
  692.0±55.0 °C(Predicted)
• 密度：
  1.352±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  31
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  90.6
• 氢给体数：
  3
• 氢受体数：
  6

文献信息

• [EN] POLYMORPHIC FORM OF PITAVASTATIN CALCIUM<br/>[FR] FORME POLYMORPHIQUE DE CALCIUM DE PITAVASTATINE
  申请人：FARMA GRS D O O

  公开号：WO2013037838A1

  公开（公告）日：2013-03-21

  The present invention relates to a new polymorphic form of pitavastatin calcium, a process for its preparation and a pharmaceutical composition comprising it. The new polymorphic form is characterized by an X-ray powder diffraction pattern as shown in Figure 1.

  本发明涉及一种匹伐他汀钙的新多形态形式，以及其制备方法和包含它的药物组合物。这种新多形态形式的特征是其X射线粉末衍射图谱如图1所示。
• PROCESS FOR PRODUCING OPTICALLY ACTIVE MEVALONOLACTONE COMPOUND
  申请人：DAICEL CHEMICAL INDUSTRIES, LTD.

  公开号：EP0747341A1

  公开（公告）日：1996-12-11

  The process for preparing mevalonolactone compounds is carried out by means of batch system chromatography or a simulated moving bed chromatographic process using columns filled with an optical resolution filler comprising a polysaccharide derivative. The simulated moving bed chromatographic process comprises forming a circulation flow circuit comprising a plurality of columns endlessly connected in series; enforcing a fluid to flow through the circuit in one direction; providing the column series alternately with an inlet port through which the fluid is introduced into the column in the flow direction and with an outlet port, through which the fluid is taken out; intermittently shifting activation of the inlet port and the outlet port in the direction of the fluid flow; introducing a solution containing a racemic mevalonolactone compound and an eluent through an inlet port into the circuit; and simultaneously taking out a solution rich in the weakly adsorbable substance and a solution rich in the strongly adsorbable and desorbed substance through the outlet port.

  制备甲羟戊酸内酯化合物的工艺是通过间歇系统色谱法或模拟移动床色谱法进行的，使用的色谱柱中填充了由多糖衍生物组成的光学分辨率填料。模拟移动床色谱过程包括形成一个循环流动回路，该回路由多个串联的色谱柱组成；强制流体沿一个方向流过该回路；在串联的色谱柱上交替设置一个进气口和一个出气口，前者用于将流体沿流动方向引入色谱柱，后者用于将流体排出；在流体流动方向上间歇性地改变入口端口和出口端口的激活；通过入口端口将含有外消旋甲戊内酯化合物和洗脱液的溶液引入回路；同时通过出口端口取出富含弱吸附物质的溶液和富含强吸附和脱附物质的溶液。
• DRUG FORMULATION CONTAINING FIBRATE MEDICAMENT AND PROCESS FOR PRODUCING THE SAME
  申请人：ASKA Pharmaceutical Co., Ltd.

  公开号：EP2047851A1

  公开（公告）日：2009-04-15

  A preparation (pharmaceutical composition) reducing a concentration of a free fatty acid and/or fibrinogen in the blood is prepared. The preparation contains a statin agent comprising at least a statin compound having a benzopyridine skeleton (e.g., pitavastatin) and a fibrate agent (e.g., fenofibrate). The preparation is useful as a preventive or treating agent for hyper-free fatty acidemia, metabolic syndrome, or type II diabetes.

  一种降低血液中游离脂肪酸和/或纤维蛋白原浓度的制剂（药物组合物）被制备出来。该制剂含有一种他汀类药物，至少包括一种具有苯并吡啶骨架的他汀类化合物（如匹伐他汀）和一种纤维酸盐制剂（如非诺贝特）。该制剂可作为高游离脂肪酸血症、代谢综合征或 II 型糖尿病的预防或治疗药物。
• Process for preparation of a quinolinecarbaldehyde
  申请人：——

  公开号：US20040147750A1

  公开（公告）日：2004-07-29

  A process for producing 2-cyclopropyl-4-(4-fluorophenyl)-quinoline-3-carbaldehyde important as intermediate for the synthesis of pharmaceuticals, efficiently from an unnecessary antipode, is provided. A process for producing 2-cyclopropyl-4-(4-fluorophenyl)-quinoline-3-carbaldehyde represented by the formula (III): 1 which comprises treating a compound represented by the formula (I) or (II): 2 (wherein A is —CHOH or —C(O)—, and R is a hydrogen atom, a C 1-4 alkyl group which may be branched, a phenyl group, an alkali metal ion or an alkaline earth metal ion) with ozone, followed by reduction with an inorganic sulfur compound or by hydrogenation for reduction decomposition.

  本发明提供了一种生产 2-环丙基-4-(4-氟苯基)-喹啉-3-甲醛的工艺，该工艺作为合成药物的重要中间体，可有效地从不必要的反式中分离出来。 一种生产式 (III) 所代表的 2-环丙基-4-(4-氟苯基)-喹啉-3-甲醛的工艺： 1 其中包括处理式 (I) 或 (II) 所代表的化合物： 2 (其中 A 为-CHOH 或-C(O)-，R 为氢原子、C 1-4 烷基（可为支链）、苯基、碱金属离子或碱土金属离子），然后用无机硫化合物还原或氢化还原分解。
• Method for preparing a 7-quinolinyl-3, 5-dihydroxyhept-6-enoate
  申请人：Tokunaga Kenichi

  公开号：US20050014947A1

  公开（公告）日：2005-01-20

  A method for preparing a 7-quinolynyl-3,5-dihydroxyhept-6-enoate useful as an intermediate for pharmaceuticals, in high yield and in high purity, is presented. It is a method for preparing a 7-quinolinyl-3,5-dihydroxyhept-6-enoate represented by the formula (IV): (wherein R represents an alkyl group or an aryl group), characterized in that a compound represented by the formula (I): (wherein R is as defined above), or a compound represented by the formula (II): (wherein R is as defined above), is reduced by sodium borohydride in the presence of a boron compound represented by the formula (III): R′OBR″ 2 (III) (wherein R′ and R″ represent independently an alkyl group), and then the resultant reaction mixture is treated with an aqueous solution of hydrogen peroxide.

  本发明提出了一种高产率和高纯度制备 7-喹啉基-3,5-二羟基庚-6-烯酸 酯的方法，这种 7-喹啉基-3,5-二羟基庚-6-烯酸酯可用作药物中间体。这是一种制备由式（IV）代表的 7-喹啉基-3,5-二羟基庚-6-烯酸酯的方法： (其中 R 代表烷基或芳基）的化合物的方法，其特征在于由式（I）： (其中 R 如上定义）或式（II）代表的化合物： 式(I)代表的化合物（其中 R 如上定义），或式(II)代表的化合物（其中 R 如上定义），在式(III)代表的硼化合物存在下被硼氢化钠还原： R′OBR″ 2 (III) (其中 R′ 和 R″ 独立地代表一个烷基），然后用过氧化氢水溶液处理生成的反应混合物。