(3R,5S,6E)-7-[4-(4-Fluorophenyl)-2-(N-Methylmethanesulfonamido)-6-(Isopropyl)Pyrimidine-5-Yl]-3,5-Dihydroxyhept-6-Enoic Acid Isopropylamine置于sodium Hydroxide,水体系中,用 乙醇 用作溶剂,化学反应 2.0H,反应生成罗伐他汀 参考文献: Crystalline Ammonium Salts Of Rosuvastatin[fr] Sels D'Ammonium Cristallins De La Rosuvastatine 标题: Crystalline Ammonium Salts Of Rosuvastatin[fr] Sels D'Ammonium Cristallins De La Rosuvastatine 摘要:提供的是罗伐他汀的烷基铵晶体盐,可用于纯化罗伐他汀及其药用可接受盐.
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:WO-2014140006-A1 优先权日:2013-03-11 标 题:Process for enantioselective synthesis of 3-hydroxy-glutaric acid monoesters and use thereof 发明人:KÖNIG BURGHARD; WETTERICH FRANK; GRÖGER HARALD; METZNER RICHARD 权利人:SANDOZ AG; UNIVERSITÄT BIELEFELD 摘要:The present invention relates to a process for the enzymatic enantioselective synthesis of 3-hydroxy- glutaric acid esters of formula 1 with R 1 being alkyl, aryl, or substituted alkyl, as well as the use compounds of formula 1 in the 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:US-10173993-B2 优先权日:2015-12-09 标题 :Process for the synthesis of sulfones and sulfonamides 发明人:VON WOLFF NIKLAS; CHAR JOËLLE; CANTAT THIBAULT 权利人:COMMISSARIAT ENERGIE ATOMIQUE 摘要:A one pot single step process is described for the synthesis of a compound, including a labeled compound, containing a sulfonyl functional group comprising the step of mixing together a silane, an SO 2 source, an electrophilic compound, an activating compound and optionally a metal catalyst. A process for producing tracers from a labeled sulfonyl containing compound prepared by the described process is also included.
1: Li M, Noordam R, Trompet S, Winter EM, Jukema JW, Arbous MS, Rensen PCN, Kooijman S. The impact of statin use on sepsis mortality. J Clin Lipidol. 2024 Jul 27:S1933-2874(24)00215-0. doi: 10.1016/j.jacl.2024.07.006. Epub ahead of print. 72(9):64-72. doi: 10.59556/japi.72.0622. 325:125123. doi: 10.1016/j.saa.2024.125123. Epub ahead of print.
合成参考文献
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