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.
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.
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: