CAS: 147511-69-1; (3R,5S,E)-7-(2-Cyclopropyl-4-(4-Fluorophenyl)Quinolin-3-yl)-3,5-Dihydroxyhept-6-Enoic Acid

该化合物是一种高纯度的Satin化合物,主要用作脂质低温剂,它作为HMG-CoA再释放酶的具有竞争力的抑制剂,有效减少胆固醇生物合成物.产品高纯度(>90%) 保证研究和药物应用的一贯性. Pitavastastatin 展示了有效的LDL-胆固醇减少,同时展示了有利的药用植物特性,包括最小的细胞化P450新陈代谢,减少了潜在的药物-药物相互作用.其稳定性和特征特征使其适合于分析和配方研究.该化合物提供了详细的高质量文件,包括HPLC和NMR验证,以支持严格的科学用途.建议在建议的条件下进行适当的处理和储存,以保持完整性.

结构式图片

MSDS等安全信息

上下游产品

heptan-2-exo-yl (3S,5R,6E)-7--3,5-dihydroxy-6-heptenoate(4R)-4,7,7-trimethyl-3-exo-(1-naphthyl)bicyclo2.2.1heptan-2-exo-yl (3S,5R,6E)-7-2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl-3,5-dihydroxy-6-heptenoate (+/-)-E-3,5-dihydroxy-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-6-heptenoic acid ethyl ester 2-cyclopropyl-4-(4-fluorophenyl)-3-(hydroxymethyl)quinoline 2-cyclopropyl-4-(4-fluorophenyl)-3-formylquinoline-3,5-dihydroxy-6-heptenoic acid ,15-lactone(3S,5R,6E)-7-2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl-3,5-dihydroxy-6-heptenoic acid ,15-lactone (E)-(3R,5S)-7-[2-cyclopropyl-4-(4-fluoro-phenyl)-quinolin-3-yl]-3,5-dihydroxy-hept-6-enoic acid ethyl ester

合成工艺路线路线简述

    匹伐他汀乙酯 反应生成匹伐他汀酸
    参考文献:Quinoline Type Mevalonolactones
    标题:Quinoline Type Mevalonolactones
    摘要:该化合物的化学式为##str1## Z=--Ch(Oh)--Ch.Sub.2--Ch(Oh)--Ch.Sub.2--Coo.1/2Ca,具有抑制hmg-Coa的作用,因此可用作胆固醇生物合成抑制剂.该化合物可以制备成药物,用于降低高脂血症,高脂蛋白血症或动脉粥样硬化.

    海关参考信息

    专利信息


    专利号:US-8269001-B2
    优先权日:2005-10-05
    标题 :Process for the synthesis of HMG-CoA reductase inhibitors
    发明人:CASAR ZDENKO
    权利人:CASAR ZDENKO; LEK PHARMACEUTICALS
    摘要:A novel synthesis of statins uses Wittig reaction of a heterocyclic core of statin with a lactonized side chain already possessing needed stereochemistry. Any separation of diastereoisomers is performed early in the course of synthesis.

    专利号:US-9085538-B2
    优先权日:2010-07-26
    标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof
    发明人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO
    权利人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO; LEK PHARMACEUTICALS
    摘要:The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.

    专利号:US-10005720-B2
    优先权日:2013-04-05
    标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
    发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
    权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
    摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

    专利号:EP-2017267-A1
    优先权日:2007-07-16
    标 题:Synthesis of statins
    发明人:KOPITAR GREGOR; MRAK PETER; OSLAJ MATEJ
    权利人:LEK PHARMACEUTICALS
    摘要:The process for synthesis of statins is presented where the intermediate intermediate (4 R ,6 S )-6-(dialkoxymethyl)tetrahydro-2 H -pyran-2,4-diol which already possesses the desired stereochemistry corresponding to final statin is prepared by an aldolaze.

    专利号:EP-2465936-A1
    优先权日:2010-12-20
    标题 :Enzymatic synthesis of statins and intermediates thereof
    权利人:LEK PHARMACEUTICALS
    摘要:The present invention discloses a process for preparing an active pharmaceutical ingredient (API) or intermediates thereof, notably particular step in the synthesis of an intermdiate useful for example in the preparation of statins, by using an enzyme capable of catalyzing oxidation or dehydrogenation. The invention further provides an expression system effectively translating said enzyme. In addition, the invention relates to a specific use of such enzyme for preparing API or intermediate thereof, and in particular for preparing statin or interemediate thereof.

    专利号:US-8471045-B2
    优先权日:2007-04-03
    标题 :Synthesis of statins
    发明人:CASAR ZDENKO; MESAR TOMAZ; KOPITAR GREGOR; MRAK PETER; OSLAJ MATEJ
    权利人:CASAR ZDENKO; MESAR TOMAZ; KOPITAR GREGOR; MRAK PETER; OSLAJ MATEJ; LEK PHARMACEUTICALS
    摘要:The process for the synthesis of statins featuring the use of an early intermediate (4R,6S)-6-(dialkoxymethyl)tetrahydro-2H-pyran-2,4-diol which already possesses the desired stereochemistry corresponding to the final statin.
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    主要参考文献


    1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Pitavastatin. 2021 Dec 1. 6(6):CD012735. doi: 10.1002/14651858.CD012735.pub2.
    3: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Pitavastatin. 2025 Sep 15. 59(2):239-52. doi: 10.1111/j.1742-1241.2005.00461.x. 29(2):137-144. doi: 10.1007/s40292-021-00496-0. Epub 2022 Jan 22. 17(2):157-168. doi: 10.1007/s40256-017-0213-8. 2025 Jan–. 12(3):271-6. doi: 10.1016/S1567-5688(11)70886-8. 20(1):103-113. doi: 10.1080/14656566.2018.1544243. Epub 2018 Nov 27.
    27:e1-e9. doi: 10.1016/j.atherosclerosissup.2017.05.001. Epub 2017 May 19. 21(1):82. doi: 10.1186/s12933-022-01524-6.

    合成参考文献


    摘要:National Library of Medicine's Medical Subject Headings. Pitavastatin. Online file (MeSH, 2016). Available from, as of November 1, 2016:
    摘要:Alberton M et al; QJM 105 (2): 145-57 (2012)
    摘要:O'Neil, M.J. (ed.). The Merck Index - An Encyclopedia of Chemicals, Drugs, and Biologicals. Cambridge, UK: Royal Society of Chemistry, 2013., p. 1394
    摘要:NIH; DailyMed. Current Medication Information for Livalo (Pitavastatin Calcium) Tablet, Film-coated (Updated: October 2013). Available from, as of November 1, 2016:
    摘要:
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