CAS: 81093-37-0; (3R,5R)-3,5-Dihydroxy-7-((1S,2S,6S,8S,8Ar)-6-Hydroxy-2-Methyl-8-(((S)-2-Methylbutanoyl)Oxy)-1,2,6,7,8,8A-Hexahydronaphthalen-1-yl)Heptanoic Acid

上下游产品

3,5-bis-epi-compactin mevastatin pravastatin sodium saltpravastatin lactone (S)-2-Methyl-butyric acid (1S,3R,4aS,7S,8S,8aS)-8-[(3R,5S)-7-(tert-butyl-diphenyl-silanyloxy)-3,5-dihydroxy-heptyl]-3-hydroxy-7-methyl-decahydro-naphthalen-1-yl ester (S)-2-Methyl-butyric acid (1S,4aS,7S,8S,8aS)-8-(2-{(4R,6S)-6-[2-(tert-butyl-diphenyl-silanyloxy)-ethyl]-2,2-dimethyl-[1,3]dioxan-4-yl}-ethyl)-7-methyl-3-oxo-decahydro-naphthalen-1-yl ester (S)-2-Methyl-butyric acid (1S,3R,4aS,7S,8S,8aS)-8-(2-{(4R,6S)-6-[2-(tert-butyl-diphenyl-silanyloxy)-ethyl]-2,2-dimethyl-[1,3]dioxan-4-yl}-ethyl)-3-hydroxy-7-methyl-decahydro-naphthalen-1-yl ester

Pravastatin Sodium Salt置于盐酸体系中,用 二氯甲烷,水 作为反应溶剂,以4.54G的收率获得产物普伐他汀
参考文献:他汀含氟衍生物及其用途
标题:他汀含氟衍生物及其用途
摘要:本发明属于药物化学领域,提供了一种3‑羟基‑3‑甲基戊二酞辅酶a还原酶抑制剂,是一种含有3‑氟‑己内酯片段及其内酯开环后形成的3‑氟‑5‑羟基戊酸及其盐或酯的他汀含氟修饰物,其结构式如下这类化合物经测试具有抑制hmg‑coa还原酶活性的效果,可作为新一代的潜在hmg‑coa还原酶抑制剂.

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-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

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-4739073-A
优先权日:1983-11-04
标题:Intermediates in the synthesis of indole analogs of mevalonolactone and derivatives thereof
发明人：KATHAWALA FAIZULLA G
权利人:SANDOZ PHARMACEUTICALS CORP
摘要:Compounds of the formula wherein one of R and Ro is and the other is primary or secondary C1-6alkyl not containing an asymmetric carbon atom, C3-6cycloalkyl or phenyl(CH2)m-, wherein R4 is hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C1-3alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R5 is hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R5a is hydrogen, C1-2alkyl, C1-2alkoxy, fluoro or chloro, and m is 1, 2 or 3, with the provisos that both R5 and R5a must be hydrogen when R4 is hydrogen, R5a must be hydrogen when R5 is hydrogen, not more than one of R4 and R5 is trifluoromethyl, not more than one of R4 and R5 is phenoxy, and not more than one of R4 and R5 is benzyloxy, R2 is hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C3-6cycloalkyl, C1-3alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R3 is hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, with the provisos that R3 must be hydrogen when R2 is hydrogen, not more than one of R2 and R3 is trifluoromethyl, not more than one of R2 and R3 is phenoxy, and not more than one of R2 and R3 is benzyloxy, X is -(CH2)n- or -CH=CH-, wherein n is 0, 1, 2 or 3, and Z is wherein R6 is hydrogen or C1-3alkyl, and R7 is hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, benzyl or M, wherein M is a pharmaceutically acceptable cation, the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level, and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.

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.