CAS: 106685-40-9; 6-(3-(Adamantan-1-yl)-4-Methoxyphenyl)-2-Naphthoic Acid

上下游产品

CAS号951645-46-8 2-Naphthaleneca... | CAS号459423-32-6 3-(1-金刚烷)-4-甲氧基苯基硼酸 | CAS号5773-80-8 6-溴-2-萘甲酸 | CAS号106685-41-0 6-[3-(1-金刚烷基)-4... | CAS号124-38-9 二氧化碳 | CAS号104224-68-2 2-(1-金刚烷基)-4-溴苯酚 | CAS号768-95-6 1-金刚烷醇 | CAS号104224-63-7 2-(1-金刚烷基)-4-溴苯甲醚 | CAS号106-41-2 对溴苯酚 | CAS号33626-98-1 6-溴-2-萘甲酸甲酯

二氧化碳置于正丁基锂,Sodium Hydride,盐酸,水体系中,用 四氢呋喃,正己烷 用作溶剂,化学反应 2.34H,以30%的收率获得阿达帕林
参考文献:Wo2007/63522
标题:Wo2007/63522

专利信息

专利号:US-12221452-B2
优先权日:2017-10-04
标题:Synthesis of cantharidin
发明人：DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R
权利人:VERRICA PHARMACEUTICALS INC
摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).

专利号:US-6521814-B1
优先权日:1997-12-22
标题:Use of ligands for treatment of diseases responsive to retinoids
发明人：CHAMBON PIERRE; BORRELLI EMILIANA; GHYSELINCK NORBERT B; DUPE VALERIE; MARK MANUEL; METZGER DANIEL
权利人:INST NAT SANTA ET DE LA RECH M; CENTRE NAT RECH SCIENT; UNIV PASTEUR; BRISTOL MYERS SQUIBB CO
摘要:The invention relates to methods for treatment of neurological disease by administering an agent which interacts with a retinoid receptor associated with the neurological disease. The invention is also related to a method of modulating dopamine receptor synthesis by introducing an agent that interacts with a retinoid receptor associated with the dopamine receptor synthesis. The invention is further related to a transgenic animal, e.g., mouse, and mammalian cell line, which is deficient in the normal synthesis of one or more receptors of RARα, β, γ and RXR, and cell line thereof.

专利号:US-8119835-B2
优先权日:2006-12-28
标 题:Method for preparation of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphtoic acid
发明人：KALVINSH IVARS; CHERNOBROVIJS ALEKSANDRS; TRIBULOVICH VYACHESLAV; LABEISH VLADIMIR
权利人:KALVINSH IVARS; CHERNOBROVIJS ALEKSANDRS; TRIBULOVICH VYACHESLAV; LABEISH VLADIMIR; JSC GRINDEKS
摘要:A method for preparation of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid is disclosed based on “one potâ€? synthesis approach including a direct synthesis of boronic acid derivative from 2-(1-adamantyl)-4-bromoanisole and cycloboranes with a subsequent Suzuki-Miyaura coupling with 6-halonaphtenoates and basic hydrolysis of the reaction product in ethylene glycol or 1,2-propanediol.

专利号:US-8106031-B2
优先权日:2006-05-02
标题:Hydrolytically-resistant boron-containing therapeutics and methods of use
发明人：LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A
权利人:LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A; ANACOR PHARMACEUTICALS INC
摘要:Compositions and methods of use of boron derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by fungi, yeast, bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.

专利号:US-2010113816-A1
优先权日:2006-12-29
标题:Method for prepartion of substituted adamantylarymagnesium halides
发明人：KALVINSH IVARS; CHERNOBROVIJS ALEKSANDRS; TRIBULOVICH VYACHESLAV; LABEISH VLADIMIR
权利人:KALVINSH IVARS; CHERNOBROVIJS ALEKSANDRS; TRIBULOVICH VYACHESLAV; LABEISH VLADIMIR
摘要:The present invention concerns fine organic synthesis, particularly the method for preparing of substituted adamantylarylmagnesium halides. n The known methods for preparing Grignard's reagent from substituted adamantylarylhalide give very low yeld of the desired product. Substituted adamantylarylhalides are active intermediates that by interacting with various electrophiles provide for a wide range of biologically active compounds. n The aim of current invention was to develop a method for preparing substituted adamantylarylmagnesium halides. The aim was attained adding lithium chloride in the Grignard's reagent synthesis by acting on is magnesium metal in dry tetrahydrofuran under argon by substituted adamantylarylhalide. n It was demonstrated that adding lithium chloride to adamantylarylhalide within a range from 1:1 to 1:2 provides for stable high yield of the desired end product.

专利号:US-8183409-B2
优先权日:2004-05-06
标题:High yield and rapid synthesis methods for producing metallo-organic salts
发明人：CHRISTGAU STEPHAN; ANDERSEN JENS E T
权利人:CHRISTGAU STEPHAN; ANDERSEN JENS E T; OSTEOLOGIX AS
摘要:A new method for preparing salts of metal cations and organic acids, especially divalent salts of alkaline earth metal ions from group II of the periodic system and carboxylic acids. The method comprising the use of a high temperature (about 90° or more) and, optionally. high pressure, in order to obtain a higher yield, purity and faster reaction speed than obtained with known synthesis methods. In particular, the present invention relates to the production of strontium salts of carboxylic acids. Novel strontium salts are also provided by the present method.