CAS: 28920-43-6; (9H-Fluoren-9-yl)Methyl Carbonochloridate

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Fmoc置于氯化亚砜体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 2.0H,反应生成氯甲酸-9-芴基甲酯
参考文献:Reversal Of P-Gp And Bcrp-Mediated Mdr By Tariquidar Derivatives
标题:Reversal Of P-Gp And Bcrp-Mediated Mdr By Tariquidar Derivatives
摘要:With An Aim To Generate Non-Toxic,Specific And Highly Potent Multidrug Resistance (Mdr) Modulators,A Novel Series Of Anthranilic Acid Amide-Substituted Tariquidar Derivatives Were Synthesized. The New Compounds Were Evaluated For Their Cytotoxicity Toward Normal Human Colon Fibroblasts (Ccd18-Co),Human Gastric Epithelial Cell Line (Hfe) And Primary Rat Liver Cells,And For Their Ability To Inhibit P-Gp/bcrp-Mediated Drug Efflux And Reversal Of P-Gp And Bcrp-Mediated Mdr In Parental And Drug-Resistant Cancer Cell Lines (Lcc6 Mdr1,Mcf-7 Flv1000,R-Hepg2,Sw620-Ad300). While Tariquidar Is Highly Toxic To Normal Cells,The New Derivatives Exhibited Much Lower Or Negligible Cytotoxicity. Some Of The New Tariquidar Derivatives Inhibited Both P-Gp And Bcrp-Mediated Drug Efflux Whereas A Few Of Them Bearing A Sulfonamide Functional Group (1,5,And 16) Are Specific To P-Gp. The New Compounds Were Also Found To Potentiate The Anticancer Activity Of The Transporter Substrate Anticancer Drugs In The Corresponding Transporter-Overexpressing Cell Lines. The Extent Of Resistance Reversal Was Found To Be Consistent With The Transporter Inhibitory Effect Of The New Derivatives. To Further Understand The Mechanism Of P-Gp And Bcrp Inhibition,The Tariquidar Derivatives Were Found To Interact With The Transporters Using An Antibody-Based Uic2 Or 5D3 Shift Assay. Moreover,The Transporters-Inhibiting Derivatives Were Found To Modulate The Atpase Activities Of The Two Mdr Transporters. Our Data Thus Advocate Further Development Of The New Compounds For The Circumvention Of Mdr. (C) 2015 Elsevier Masson Sas. All Rights Reserved.
Doi:10.1016/j.Ejmech.2015.06.049

专利信息

专利号:US-9920084-B2
优先权日:2011-08-23
标题 :Ionic tags for synthesis of oligoribonucleotides
发明人：DAMHA MASAD J; HASSLER MATTHEW; CHAN TAK-HANG; NANDYALA MALLIKARJUNA REDDY; DONGA ROBERT ALEXANDER
权利人:DAMHA MASAD J; HASSLER MATTHEW; CHAN TAK HANG; NANDYALA MALLIKARJUNA REDDY; DONGA ROBERT ALEXANDER; THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING/MCGILL UNIV; HONG KONG POLYTECHNIC UNIV
摘要:The invention relates to the chemical synthesis of oligonucleotides, e.g., oligoribonucleotides. In another aspect, the invention relates to compounds of formula (II) processes for making these compounds, and the use thereof in the chemical synthesis of oligonucleotides, e.g., oligoribonucleotides. The invention also relates to methods of synthesis of oligomers, including but not limited to oligopeptides, oligosaccharides and oligonucleotides, particularly oligoribonucleotides and also oligodeoxyribonucleotides, in solution systems, and ionic tag linkers for use in methods provided herein.

专利号:US-6683189-B1
优先权日:1996-02-26
标 题 :Method for the synthesis of pyrrole and imidazole carboxamides on a solid support
发明人：DERVAN PETER B; BAIRD ELDON
权利人:CALIFORNIA INST OF TECHN
摘要:The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.

专利号:US-11466050-B2
优先权日:2014-09-29
标 题 :Method for peptide synthesis and apparatus for carrying out a method for solid phase synthesis of peptides
发明人：KNAUER SASCHA; ROESE TOBIAS MICHAEL LOUIS; AVRUTINA OLGA; KOLMAR HARALD; UTH CHRISTINA
权利人:SULFOTOOLS GMBH
摘要:The invention relates to a method for peptide synthesis, wherein said method comprises the steps of reacting a first amino acid or a first peptide with an α-amine protected second amino acid in a solvent selected from the group consisting of water, alcohol, and a mixture of water and alcohol, and removing the α-amine protecting group with a deprotecting solution. The invention further relates to protective agents, their use and an apparatus for carrying out a method for solid phase synthesis of peptides.

专利号:US-2004058888-A1
优先权日:2000-01-13
标题:Methods for synthesis of alpha-d-gal (1~>3) gal-containing oligosaccharides
发明人：BORNAGHI LAURENT; DEKANY GYULA; DRINNAN NICHOLAS BARRY; PAPAGEORGIOU JOHN; WEST MICHAEL LEO
摘要:This invention relates to reagents and methods for synthesis of biologically active di- and tri-saccharides comprising α-D-Gal(1→3)-D-Gal. In particular the invention provides novel reagents, intermediates and processes for the solution or solid phase synthesis of α-D-galactopyranosyl-(1→3)-D-galactose, and derivatives thereof. In one preferred embodiments the invention provides a protected monosaccharide building block of general formula (II): in which R 3 is methoxy or methyl; R 1 is H, benzoyl, pivaloyl, 4-chlorobenzoyl, acetyl, chloroacetyl, levulinoyl, 4-methylbenzoyl, benzyl, 3,4-methylenedioxybenzyl, 4-methoxybenzyl, 4-chlorobenzyl, 4-acetamidobenzyl, or 4-azidobenzyl; and R 2 is H, Fmoc, benzoyl, pivaloyl, 4-chlorobenzoyl, acetyl, chloroacetyl, levulinoyl, 4-methylbenzoyl, benzyl, 3,4-methylenedioxybenzyl, 4-methoxybenzyl, 4 -chlorobenzyl, 4-acetamidobenzyl, or 4-azidobenzyl.

专利号:US-6048975-A
优先权日:1991-09-12
标 题:Process for the chemical synthesis of oligonucleotides
发明人：PFLEIDERER WOLFGANG; BERGMANN FRANK
权利人:HOECHST AG
摘要:A process for the chemical synthesis of oligonucleotides n Use of a dansylethoxycarbonyl group as base-labile 5'-hydroxyl protective group in the chemical synthesis of DNA and RNA and suitable synthetic processes. n The ease of detection of the dansyl protective group and the ease of elimination from the sugar residue of the nucleotide without side reactions make oligonucleotide synthesis possible with high yields in very small quantities.

专利号:US-7825244-B2
优先权日:2005-06-10
标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis
发明人：BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG
权利人:JANSSEN PHARMACEUTICA NV
摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.