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(3R,5S,6E)-7-(4-对氟苯硫基-6,7,8-三氟喹啉-3-基)-3,5-二羟基庚烯酸钙有关物质的合成 被引量：1

Synthesis of the Related Substances of Calcium(3R,5S,6E)-7-[4-(4-Fluorophenylthio)-6,7,8-trifluoroquinolin-3-yl]-3,5-dihydroxyheptenoate
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摘要 为加强对降血脂候选药物(3R,5S,6E)-7-(4-对氟苯硫基-6,7,8-三氟喹啉-3-基)-3,5-二羟基庚烯酸钙(2)的质量控制,合成了可能存在于药品中的5个有关物质:(3R,6E)-7-(4-对氟苯硫基-6,7,8-三氟喹啉-3-基)-3-羟基-5-氧代庚烯酸(3)、(3R,5S,6E)-7-(4-对氟苯亚磺酰基-6,7,8-三氟喹啉-3-基)-3,5-二羟基庚烯酸(4)、(3R,5S,6Z)-7-(4-对氟苯硫基-6,7,8-三氟喹啉-3-基)-3,5-二羟基庚烯酸(5)、(3R,5R,6E)-7-(4-对氟苯硫基-6,7,8-三氟喹啉-3-基)-3,5-二羟基庚烯酸(6),以及(3R*,5S*,6E)-7-(4-对氟苯硫基-6,7,8-三氟喹啉-3-基)-3,5-二羟基庚烯酸(7)。 Five related substances of calcium（3R,5S,6E）-7-[4-（4-fluorophenylthio）-6,7,8-trifluoroquinolin- 3-yl]-3,5-dihydroxyheptenoate（2）which is in extensively preclinical investigation as an anti-hypercholesterolemic drug candidate,were synthesized and may be served as references in the quality control of 2.They were（3R,6E） - 7-[4-（4-fluorophenylthio）-6,7,8-trifluoroquinolin-3-yl]-3-hydroxy-5-oxoheptenoic acid（3）,（3R,5S,6E）-7- [4-（4-fluorophenylsulfinyl）-6,7,8-trifluoroquinolin-3-yl]-3,5-dihydroxyheptenoic acid（4）,（3R,5S,6Z）-7-[4- （4-fluorophenylthio）-6,7,8-trifluoroquinolin-3-yl]-3,5-dihydroxyheptenoic acid（5）,（3R,5R,6E）-7-[4-（4- fluorophenylthio）-6,7,8-trifluoroquinolin-3-yl]-3,5-dihydroxyheptenoic acid（6）,and（3R~＊,5S~＊,6E）-7-[4-（4- fluorophenylthio） -6,7,8-trifluoroquinolin-3-yl]-3,5-dihydroxyheptenoic acid（7）.
作者 郝群 蔡正艳 潘竞 李泳佳 周伟澄
机构地区 上海医药工业研究院
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2010年第12期884-890,共7页 Chinese Journal of Pharmaceuticals
基金 国家“重大新药创制”科技重大专项(2009ZX09301-007) 上海创新行动计划(09431901300)
关键词 降血脂药物 HMG COA还原酶抑制剂 有关物质 合成 anti-hypercholesterolemic drug HMG CoA reductase inhibitor related substance synthesis
分类号 O626 [理学—有机化学]
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参考文献12

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二级参考文献12

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共引文献11

同被引文献4

  • 1谢沐风.如何建立高效液相色谱法测定有关物质的方法[J].中国医药工业杂志,2007,38(1):45-48. 被引量：62
  • 2Cai Z,Zhou W,Sun L. Synthesis and HMG CoA reductase inhibition of 4-thiophenyl quinolines as potential hypocholesterolemic agents[J].Bioorganic and Medicinal Chemistry Letters,2007,(24):7809-7829.
  • 3Cai Z,Zhou W,Pan J. Synthesis of4-phenoxy quinoline mevalonolactones and evaluation of their HMG CoA reductase inhibition activities[J].J Chin Pharmaceu Sci,2010,(01):15-23.
  • 4Hao Q,Cai Z,Pan J. Synthesis and anti-hypercholesterolemic evaluations of calcium salts of 4-substituted quinolinebased mevalonic acid[J].CHEMICAL BIOLOGY & DRUG DESIGN,2011,(04):730-733.

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中国医药工业杂志
2010年 第12期

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