📜亚氨基芪置于silver Trifluoroacetate体系中,用 甲醇,二氯甲烷 用作溶剂,以94%的收率获得吖啶 参考文献:Formation Of Acridine From The Reaction Of Dibenz[b,F]Azepine With Silver(I); Formation Of An Aromatic Nitrenium Ion 标题:Formation Of Acridine From The Reaction Of Dibenz[b,F]Azepine With Silver(I); Formation Of An Aromatic Nitrenium Ion 摘要: Doi:10.1021/jo00240A040
专利号:US-8822702-B2 优先权日:2002-12-20 标 题 :Synthesis of amines and intermediates for the synthesis thereof 发明人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL 权利人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL; BASF SE 摘要:The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, n nor especially of amides of the formula II,n n nwherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.
专利号:WO-9624694-A1 优先权日:1995-02-10 标 题:Method and kit for fluorometric analysis of enzymes catalyzing synthesis of nucleic acids 发明人:CHAVAN SURENDRA J; PROCHASKA HANS J 权利人:SLOAN KETTERING INST CANCER 摘要:This invention provides a method for detecting in a sample an enzyme which catalyzes the synthesis of a double-stranded nucleic acid molecule from a nucleic acid template which comprises contacting the sample with a suitable fluorophore which selectively binds to double-stranded DNA. Also provided is a method for determining in a sample the activity of such an enzyme. This invention also provides a method for detecting an RNA-DNA heteroduplex in a sample which comprises contacting the sample with a suitable fluorophore which selectively binds to double-stranded DNA. This method for detecting an RNA-DNA heteroduplex may further comprise quantitatively determining detected RNA-DNA heteroduplex. This invention also provides a method for detecting in a sample en enzyme which catalyzes the synthesis of and RNA-DNA heteroduplex from a nucleic acid template, as well as a method of detecting the activity of such an enzyme in a sample. This invention further provides a method for detecting the viral load of HIV in a sample. Also provided is a method for diagnosing an HIV infection in a subject, and for monitoring the progression of an HIV infection in a subject. Also provided is a method for determining the viral load of HIV in a subject infected with HIV. This invention further provides a method for identifying whether a substance inhibits reverse transcriptase. Finally, this invention provides a kit for assaying an enzyme which catalyzes the synthesis of a double-stranded nucleic acid molecule from a nucleic acid template.
专利号:US-8642809-B2 优先权日:2007-09-25 标 题:Methods of synthesis of certain hydroxamic acid compounds 发明人:REISCH HELGE A; LEEMING PETER; RAJE PRASAD S 权利人:REISCH HELGE A; LEEMING PETER; RAJE PRASAD S; TOPOTARGET UK LTD 摘要:The present invention pertains to the general field of chemical synthesis, and more particularly to methods for the synthesis of certain hydroxamic acid compounds, and in particular, (E)-N-hydroxy-3-(3-phenylsulfamoyl-phenyl)-acrylamide, also known as PXD101 and Belinostat®, comprising, for example, the steps of: (SAF) sulfonamide formation; (PUR C ) optional purification; (AAA) alkenyl-acid addition, comprising: either (i): the steps of, in order: (ACAEA) alkenyl-carboxylic acid ester addition; (PUR E ) optional purification; and (CAD) carboxylic acid deprotection; or (ii): the step of: (ACAA) alkenyl-carboxylic acid addition; (PUR F ) optional purification; (HAF) hydroxamic acid formation; and (PUR G ) optional purification.
专利号:US-9126995-B2 优先权日:2011-11-08 标题:Method for catalytic asymmetric synthesis of optically active isoxazoline compound and optically active isoxazoline compound 发明人:TOYAMA KEN-ICHI; MORIYAMA YUJI; MATOBA KAZUTAKA; YAOSAKA MANABU; IKEDA EITATSU 权利人:NISSAN CHEMICAL IND LTD 摘要:There is provided a method for catalytic asymmetric synthesis of optically active isoxazoline compound and an optically active isoxazoline compound. A method for catalytic asymmetric synthesis of optically active isoxazoline compound of a formula (6) including reacting an α,β-unsaturated carbonyl compound of a formula (1) and a hydroxylamine in a solvent in the presence of a base by adding a chiral phase transfer catalyst. An optically active isoxazoline compound of a formula (13) that can be synthesized by the method.
专利号:US-4895922-A 优先权日:1988-05-05 标 题 :Low temperature synthesis of polyesteramides 发明人:OGATA NAOYA 权利人:GOODYEAR TIRE & RUBBER 摘要:This invention disclosed a process for the synthesis of polyesteramides. By utilizing the phosphorus containing catalyst systems of the present invention, such polyesteramides can be synthesized at relatively low temperatures. The present invention specifically discloses a process for the synthesis of a polyesteramide which comprises polymerizing at least one diamine, at least one diol, and at least one dicarboxylic acid in the presence of (1) at least one acid acceptor; (2) at least one halogenated organic compound; and (3) at least one phosphorus containing compound selected from the group consisting of (a) triphenylphosphine, (b) triphenylphosphine oxide, (c) triphenylphosphine sulfide, (d) polymeric agents having pendant diphenylphosphine groups, (e) silicon-phosphorus compositions which contain at least one divalent oxygen atom which is bonded directly to a tetravalent silicon atom and a trivalent or pentavalent phosphorus atom; (f) compounds with the structural formula (C 6 H 5 ) 3 P=N-R, wherein R is a hydrogen atom or an alkyl group containing from 1 to 10 carbon atoms; and (g) compounds with the structural formula (C 6 H 5 )PR 1 R 2 wherein R 1 and R 2 can be the same or different, wherein R 1 is selected from the group consisting of alkyl groups containing from 1 to 10 carbon atoms and phenyl groups, and wherein R 2 is an alkyl group containing from 1 to 10 carbon atoms.
专利号:US-6849743-B2 优先权日:1997-08-15 标 题 :Synthesis of clasto-lactacystin β-lactone and analogs thereof 发明人:SOUCY FRANCOIS; FLAMONDON LOUIS; BEHNKE MARK; ROUSH WILLIAM 权利人:MILLENNIUM PHARM INC 摘要:The present invention is directed to an improved synthesis of clasto-lactacystin-β-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-β-lactones, and analogs thereof and their use as proteasome inhibitors.
参考文献:10.3109/10520295.2011.577097 摘要:Seema M, Punith B, Devaki N. A simple and rapid nuclear staining method for Rhizoctonia solani Kuhn. Biotechnic & Histochemistry. 2011 Jul 12;87(3):169–71. doi: 10.3109/10520295.2011.577097. 参考文献:10.1007/s00284-005-0078-y 摘要:Barreto HM, Siqueira-Junior JP. Protective effect of furocoumarins against 254-nm ultraviolet in Staphylococcus aureus. Curr Microbiol. 2006 Jan;52(1):40–4. doi: 10.1007/s00284-005-0078-y. 参考文献:10.1158/0008-5472.can-11-1218 摘要:Lovejoy DB, Jansson PJ, Brunk UT, Wong J, Ponka P, Richardson DR. Antitumor activity of metal-chelating compound Dp44mT is mediated by formation of a redox-active copper complex that accumulates in lysosomes. Cancer Res. 2011 Sep 01;71(17):5871–80. doi: 10.1158/0008-5472.can-11-1218. 参考文献:10.7150/ijms.8.387 摘要:Pipkorn R, Wiessler M, Waldeck W, Lorenz P, Muehlhausen U, Fleischhacker H, Koch M, Braun K. Enhancement of the click chemistry for the inverse Diels Alder technology by functionalization of amide-based monomers. Int J Med Sci. 2011;8(5):387–96. 参考文献:10.1371/journal.pone.0021876 摘要:Wesley CS, Guo H, Chaudhry KA, Thali MJ, Yin JC, Clason T, Wesley UV. Loss of PTB or Negative Regulation of Notch mRNA Reveals Distinct Zones of Notch and Actin Protein Accumulation in Drosophila Embryo. PLoS ONE. 2011 Jul 05;6(7):e21876. doi: 10.1371/journal.pone.0021876.