专利号:US-8309744-B2 优先权日:2008-08-29 标题:Prostaglandin synthesis and intermediates for use therein 发明人:ALBERICO DINO; CLAYTON JOSHUA; GORIN BORIS IVANOVICH; OUDENES JAN 权利人:ALBERICO DINO; CLAYTON JOSHUA; GORIN BORIS IVANOVICH; OUDENES JAN; ALPHORA RES INC 摘要:Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: n nwherein R represents an aryl group such as p-methoxyphenyl.n n This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required α-side chain and then the required ω-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.
专利号:US-6177572-B1 优先权日:1997-08-20 标题 :Solid and liquid-phase synthesis of benzoxazoles and benzothiazoles and their use 发明人:WANG FENGJIANG 权利人:SEPRACOR INC 摘要:Methods for preparing benzoxazoles and benzothiazoles on solid supports. Substituted benzothiazoles and benzoxazoles, libraries of the compounds, and methods of using the compounds are also disclosed.
专利号:WO-2009049476-A1 优先权日:2007-09-20 标题 :Process for the manufacture of (+)-biotin 发明人:CHEN FEN-ER; DAI HUI-FANG; HUANG JIAN; XIONG FEI; JING SHU-PING 权利人:DSM IP ASSETS BV; UNIV FUDAN; CHEN FEN-ER; DAI HUI-FANG; HUANG JIAN; XIONG FEI; JING SHU-PING 摘要:Disclosed are processes for preparing synthetic biotin intermediates and a process for preparing biotin using said intermediates. In particular, disclosed is a process for the stereoselective total synthesis of the natural product (+)-biotin of formula (I).
专利号:US-8653238-B2 优先权日:2006-02-27 标题:Compositions and methods for transport of molecules with enhanced release properties across biological barriers 发明人:WENDER PAUL A; GOUN ELENA A; JONES LISA R 权利人:WENDER PAUL A; GOUN ELENA A; JONES LISA R; UNIV LELAND STANFORD JUNIOR 摘要:Conjugates of a cargo molecule with a transporter molecule are disclosed, where the cargo molecule and the transporter molecule are linked covalently by a releasable linker. The cargo of the conjugate can be a biologically active agent or a reporter molecule. The transporter modulates the transport of the cargo across a biological barrier (e.g., a cell membrane) compared to the transport of the unconjugated cargo. Releasable linkers suitable for rapid and facile conjugation to various types of cargo and transporters are also disclosed, along with methods for using the linkers in the synthesis of conjugates.
专利号:US-6133452-A 优先权日:1997-08-22 标题 :Synthesis of bisindolylmalimides 发明人:FAUL MARGARET MARY; WINNEROSKI JR LEONARD LARRY 权利人:LILLY CO ELI 摘要:The present invention provides for the reaction of optionally substituted indole-3-acetamides with optionally substituted methyl indole-3-glyoxyl reagent to prepare potent PKC inhibitors. The reaction is very efficient and robust macrocyclization methodology.
专利号:US-2009264648-A1 优先权日:2008-01-14 标题:Synthesis of pyrazoles 发明人:CHEW WARREN; WANG ZHENG; CHEAL GLORIA; BERTRAND MARTIAL; POTOSKI JOHN; MIRMEHRABI MAHMOUD; NENCINI ARIANNA; ZANALETTI RICCARDO 权利人:WYETH CORP; SIENA BIOTECH SPA 摘要:The present invention provides compounds and compositions, methods of making them, and methods of using them to modulate α7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.
[参考文献]: Oleksandr Kuznetsov, Et Al. Water-Soluble Nanodiamond. Langmuir. 2012 Mar 20;28(11):5243-8. [参考文献]: Soma Chakraborty, Et Al. Functionalization Of Potassium Graphite. Angew Chem Int Ed Engl. 2007;46(24):4486-8.
合成参考文献
摘要:Shimada, K., Science of Synthesis Knowledge Updates, (2010) 1, 458. 摘要:Mourad, A. K.; Czekelius, C., Science of Synthesis Knowledge Updates, (2011) 3, 83.