棕榈酸置于碘,Zinc Trifluoromethanesulfonate体系中,用 乙腈 用作溶剂,化学反应 5.67H,反应生成棕榈酸异丙酯 参考文献:Zn(Otf)2-Promoted Chemoselective Esterification Of Hydroxyl Group Bearing Carboxylic Acids 标题:Zn(Otf)2-Promoted Chemoselective Esterification Of Hydroxyl Group Bearing Carboxylic Acids 摘要:Selective Esterification Of Aliphatic And Aromatic Carboxylic Acids With Various Alcohols Is Studied Using Triphenylphosphine,I-2,And A Catalytic Amount Of Zn(Otf)(2). Use Of This Catalyst Allows The Formation Of Esters At A Faster Rate With Good To Excellent Yield By Activating The In Situ Generated Acyloxyphosphonium Ion Intermediate. During The Esterification Process,Both Their Aromatic And Aliphatic Hydroxyl Groups Are Fully Preserved From Trans-Esterification. The Results Show That The Bulkiness And The Reactivity Of This Doubly Activated Intermediate Iii Control The Selectivity And The Rate Of The Reaction,Respectively. The Method Is Also Useful For Direct Amidation Reactions. Doi:10.1021/jo302502R
专利号:US-2014255328-A1 优先权日:2013-03-11 标 题:Hydrothermal Synthesis of Zinc Phlogopite 发明人:MCGUIRE MEAGHAN CLARK; BULL IVOR; JOHNSON GEOFFREY MARK 权利人:BASF SE 摘要:This invention relates to a synthetically derived zinc phlogopite platelets, of superior platelet diameter, effect pigments comprising such synthetically derived platelets and methods of forming said substrates. More specifically the disclosure describes an improved hydrothermal synthesis of zinc phlogopite suitable as a platelets for interference pigments, barrier and flame retardant applications.
专利号:US-7888337-B2 优先权日:2007-08-31 标 题 :Synthesis of oseltamivir containing phosphonate congeners with anti-influenza activity 发明人:WONG CHI-HUEY; FANG JIM-MIN; SHIE JIUN-JIE; CHENG YIH-SHYUN EDMOND; JAN JIA-TSRONG 权利人:ACADEMIA SINICA 摘要:Novel phosphonate compounds are described. The compounds have activity as neuraminidase inhibitors against wild-type and H274Y mutant of H1N1 and H5N1 viruses. The present disclosure also provides an enantioselective synthetic route to known neuraminidase inhibitors oseltamivir and the anti-flu drug Tamiflu®, as well as novel phosphonate compounds, via D-xylose. Another efficient and flexible synthesis of Tamiflu and the highly potent neuraminidase inhibitor Tamiphosphor was also achieved in 11 steps and >20% overall yields from the readily available fermentation product (1S-cis)-3-bromo-3,5 -cyclohexadiene-1,2-diol. Most of the reaction intermediates were obtained as crystals without tedious purification procedures. The key transformations include an initial regio- and stereoselective bromoamidation of a bromoarene cis-dihydrodiol, as well as the final palladium-catalyzed carbonylation and phosphonylation.
专利号:US-6818633-B2 优先权日:2001-06-29 标题:Antiviral compounds and methods for synthesis and therapy 发明人:BALZARINI JAN M R; DE CLERCQ ERIK D A; HOLY ANTONIN 权利人:ACAD OF SCIENCE CZECH REPUBLIC; REGA STICHTING 摘要:Novel compounds are provided having formula (I)whereR1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).
专利号:US-9597327-B2 优先权日:2005-05-25 标 题:Synthesis of (R)-N-methylnaltrexone 发明人:DOSHAN HAROLD D; PEREZ JULIO 权利人:PROGENICS PHARM INC 摘要:This invention relates to stereoselective synthesis of R-MNTX and intermediates thereof, pharmaceutical preparations comprising R-MNTX or intermediates thereof and methods for their use.
专利号:US-7598291-B2 优先权日:2004-09-02 标题 :Methods and compositions for enhancing collagen and proteoglycan synthesis in the skin 发明人:NIMNI MARCEL; HAN BO 权利人:NIMNI MARCEL; HAN BO 摘要:A composition for application to the skin can stimulate the in vivo synthesis of collagen and proteoglycans and improve the appearance of the skin, increasing its elasticity and fullness. In general, a composition according to the present invention comprises: (1) an antioxidant compound in a quantity sufficient to enhance collagen synthesis in the skin; (2) an organic penetrant in which the antioxidant compound is soluble in a sufficient quantity that a concentration of the antioxidant compound sufficient to enhance collagen synthesis can be applied topically and penetrate the skin; (3) a mixture of essential amino acids; (4) a supplemental source of sulfur; and (5) a topical pharmaceutically acceptable carrier. The antioxidant compound can be lipoic acid, a lipoic acid analogue or derivative, a bioflavonoid, a constituent of ginkgo, or an isoflavone. The organic penetrant is preferably benzyl alcohol. Other ingredients, such as esters of tocopherol and ascorbic acid, can be included.
专利号:US-2010160244-A1 优先权日:2004-09-02 标 题 :Methods and compositions for enhancing collagen, proteoglycan, and glutathione synthesis in the skin 发明人:NIMNI MARCEL; HAN BO 权利人:NIMNI MARCEL; HAN BO 摘要:A composition for application to the skin can stimulate the in vivo synthesis of collagen and proteoglycans and improve the appearance of the skin, increasing its elasticity and fullness. In general, a composition according to the present invention comprises: (1) an antioxidant compound in a quantity sufficient to enhance collagen synthesis in the skin; (2) an organic penetrant in which the antioxidant compound is soluble in a sufficient quantity that a concentration of the antioxidant compound sufficient to enhance collagen synthesis can be applied topically and penetrate the skin; (3) a mixture of essential amino acids or hydrolyzed whey protein; (4) a supplemental source of sulfur; and (5) a topical pharmaceutically acceptable carrier. The antioxidant compound can be lipoic acid or a lipoic acid analogue or derivative. The organic penetrant is preferably benzyl alcohol. Other ingredients, such as esters of tocopherol and ascorbic acid, can be included.
[参考文献]: Elder Dp, Et Al. Pharmaceutical Excipients - Quality, Regulatory And Biopharmaceutical Considerations. Eur J Pharm Sci. 2016 May 25;87:88-99. [参考文献]: Luís â, Et Al. Design And Characterization Of Bioactive Bilayer Films: Release Kinetics Of Isopropyl Palmitate. Antibiotics (Basel). 2020 Jul 24;9(8):443. [参考文献]: Amnon C Sintov, Et Al. Comparative Percutaneous Permeation Study Using Caffeine-Loaded Microemulsion Showing Low Reliability Of The Frozen/thawed Skin Models. Int J Pharm. 2014 Aug 25;471(1-2):516-24. [参考文献]: Amnon C Sintov, Et Al. Transdermal Delivery Of Curcumin Via Microemulsion. Int J Pharm. 2015 Mar 15;481(1-2):97-103. [参考文献]: Hong Guo, Et Al. Effects Of Isopropyl Palmitate On The Skin Permeation Of Drugs. Biol Pharm Bull. 2006 Nov;29(11):2324-6.
合成参考文献
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