CAS: 75330-75-5; (S)-(1S,3R,7S,8S,8Ar)-8-(2-((2R,4R)-4-Hydroxy-6-Oxotetrahydro-2H-Pyran-2-yl)Ethyl)-3,7-Dimethyl-1,2,3,7,8,8A-Hexahydronaphthalen-1-Yl 2-Methylbutanoate

上下游产品

CAS号79691-11-5 6(R)-[2-[1,2,6,... | CAS号75225-51-3 洛伐他汀钠 | CAS号79902-31-1 4-(叔丁基二甲基甲硅烷氧基)... | CAS号79902-63-9 辛伐他汀，斯伐他汀 | CAS号75225-50-2 Lovastatin Hydr... | CAS号67-64-1 丙酮 | CAS号75-65-0 叔丁醇 | CAS号109273-98-5 去羟基洛伐他汀 | CAS号75225-51-3 洛伐他汀钠 | CAS号151006-15-4 (4R,6R)-4-hydro... | CAS号132748-10-8 莫那可林J酸

Lovastatin Acid置于三氟乙酸体系中,用 乙酸乙酯 作为反应溶剂,化学反应 0.17H,反应生成 洛伐他汀
参考文献:Bioprospecting Lovastatin Production From A Novel Producer Cunninghamella Blakesleeana
标题:Bioprospecting Lovastatin Production From A Novel Producer Cunninghamella Blakesleeana
摘要:除了具有抗胆固醇的活性外,洛伐他汀在治疗各种疾病(尤其是癌症)方面的应用也受到全世界的关注.研究人员从土壤样本中分离出 36 种丝状真菌,并通过酵母生长生物测定法对其生产的洛伐他汀进行了筛选.c9 菌株(后被鉴定为 Cunninghamella Blakesleeana)被筛选为生产洛伐他汀的潜在菌株.使用 Tlc,Hptlc 和 HPLC 对化合物进行了进一步确认,分别观测到与标准洛伐他汀相似的 Rf 值,密度图峰和色谱峰.纯化后的洛伐他汀在红外分析中显示出与标准洛伐他汀相似的内酯环峰,位于 1763.63 Cm-1 处.对纯化的洛伐他汀进行进一步的结构分析,包括核磁共振和液相色谱-质谱分析,证实其分子式和分子量与标准品相似.在定量方面,C.Blakesleeana,赤曲霉和黄曲霉在未进行任何优化的情况下分别产生了1.4 Mg G-1 Dws,0.83 Mg G-1 Dws和0.3 Mg G-1 Dws的洛伐他汀(p <0.0001).洛伐他汀具有明显的抗氧化性,Ic50:145.9 µg Ml-1(140 µl),在199.5 µg/ml时抑制率最大,具有统计学意义(p <0.0001).
DOI:10.1007/s13205-018-1384-Y

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-10973847-B2
优先权日:2017-06-30
标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
发明人：JOHNSON JEREMIAH A; GOLDER MATTHEW R
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

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.