CAS: 7154-73-6; Pyrrolidinoethylamine

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65592-36-1 93564-22-8 105479-10-5

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CAS号109-99-9 四氢呋喃 | CAS号107-15-3 乙二胺 | CAS号29134-29-0 (1-吡咯)乙腈 | CAS号7250-67-1 N-(2-氯乙基)吡咯烷盐酸盐 | CAS号123-75-1 四氢吡咯 | CAS号2576-47-8 2-溴乙胺氢溴酸盐 | CAS号79315-01-8 N-(2-(pyrrolidi... | CAS号76277-38-8 2-(2-(pyrrolidi... | CAS号110-52-1 1,4-二溴丁烷 | CAS号5050-41-9 1-(2-氯乙基)吡咯烷 | CAS号356068-94-5 Z)-5-(5-氟-2-氧代-... | CAS号209968-27-4 4-溴-N-(2-吡咯烷-1-... | CAS号128368-39-8 4-phenyl-3-(2-p... | CAS号128554-85-8 2-nitro-N-(2-py... | CAS号128352-92-1 4-phenyl-3-(2-p... | CAS号122777-92-8 2-nitro-N-(2-py... | CAS号118269-78-6 4-methyl-6-phen... | CAS号69577-10-2 2-[2-(1-pyrroli... | CAS号77731-48-7 3-phenyl-1-(2-p... | CAS号65875-38-9 N-Benzyl-2-(1-p...

(2-Pyrrolidin-1-Ylethyl)Carbamic Acid Tert-Butyl Ester置于盐酸体系中,用 乙酸乙酯 作为反应溶剂,化学反应 0.5H,反应生成 1-(2-氨乙基)吡咯烷
参考文献:Thiazole Orange-Spermine Conjugate: A Potent Human Telomerase Inhibitor Comparable To Braco-19
标题:Thiazole Orange-Spermine Conjugate: A Potent Human Telomerase Inhibitor Comparable To Braco-19
摘要:In This Report,We Synthesized A Series Of To Conjugates Containing Different Amino Side Chains And Investigated Their Binding To Telomeric G-Quadruplex Dna (G4) Using Several Biophysical Methods Including Fluorometric Titration And Thermal Denaturation Monitored By Fluorescence And Circular Dichroism. The Composition Of Side Chains Strongly Affects The Binding Of These Molecules To G-Quadruplex Dna. Incorporation Of Amino Side Chains Increases The Binding Affinity Of To Toward G4 But Has A Minimal Effect On Its Selectivity For G4 Over Duplex Dna. The Plausible Binding Modes Are A Synergistic Effect Of End-Stacking And Groove Interactions As Indicated By Docking Studies. Inhibition Of Human Telomerase Activity By To Derivatives Was Determined In Vitro By The Trap Assay. Several Derivatives Can Selectively Inhibit The Activity Of Telomerase Over Dna Polymerase At Low Concentrations. More Significantly,To-Spermine Conjugate (16) Exhibits A Remarkable Effect On Telomerase Inhibition In The Submicromolar Range,Which Is Comparable To The Inhibition Effect Of A Well-Known G4 Ligand,Braco-19. Our Results Here Provide Guidance Of Utilizing To Derivatives As A Viable Scaffold To Design Novel G4 Ligands,G4 Probes,And Potent Telomerase Inhibitors. (C) 2019 Elsevier Masson Sas. All Rights Reserved.
DOI:10.1016/j.Ejmech.2019.04.041

专利信息

专利号:US-5877278-A
优先权日:1992-09-24
标题:Synthesis of N-substituted oligomers
发明人：ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA
权利人:CHIRON CORP
摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.

专利号:US-2024368099-A1
优先权日:2022-01-18
标 题:Methods for the synthesis of di(hydroxymethyl)tetrahydrofuran and its application in polyesters and polyurethanes
发明人：SPIEGELBERG BRIAN; BRANDT ADRIAN; BECK HORST; KUX ALEXANDER; TIN SERGEY; DE VRIES JOHANNES GERARDUS
权利人:HENKEL AG & CO KGAA
摘要:The present invention relates to the synthesis of di(hydroxymethyl)tetrahydrofuran (DHMTHF) and the preparation of trans-enriched mixtures of DHMTHF. The invention further refers to polyester polyols which are obtained by reaction of cis/trans DHMTHF mixtures with a dicarboxylic acid. The invention further relates to polyurethanes and compositions containing a polyester polyol comprising DHMTHF, in particular to such polyurethane-containing (adhesive) compositions.

专利号:WO-2016173960-A1
优先权日:2015-04-29
标 题 :Optimized synthesis of pregabalin and 4-aminobutane acid using an improved method for producing conjugated nitroalkenes
发明人：STUMPF MARCUS
权利人:K H S PHARMA HOLDING GMBH
摘要:The invention relates to an optimized synthesis of pregabalin and additional 4-aminobutane acids using an improved method for producing conjugated nitroalkenes. This is achieved by a nitro-aldol reaction of an aliphatic aldehyde with a nitroalkane in the presence of a suitable diamine directly followed by an elimination of the conjugated nitroalkene by adding an acid, a subsequent catalyzed asymmetrical 1,4-Michael addition of a suitable nucleophile, and a subsequent retro-Claisen reaction or a hydrolosis and decarboxylation with a concluding reduction to 4-aminobutane acid.

专利号:US-2025129021-A1
优先权日:2023-09-19
标 题:Small molecule protein synthesis modulators
发明人：GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE
权利人:INTERDICT BIO INC
摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.

专利号:US-7109377-B2
优先权日:1996-10-16
标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products
发明人：SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R
权利人:HARVARD COLLEGE
摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.

专利号:US-6121054-A
优先权日:1997-11-19
标 题 :Method for separation of liquid and solid phases for solid phase organic syntheses
发明人：LEBL MICHAL
权利人:TREGA BIOSCIENCES INC
摘要:A simple, efficient apparatus and method for separation of solid and liquid phases useful in methods of high-throughput combinatorial organic synthesis of large libraries or megaarrays of organic compounds is disclosed. The apparatus and method are useful, whether as part of an automated, robotic or manual system for combinatorial organic synthesis. In a preferred embodiment, an apparatus and method of removal of liquid phase from solid phase compatible with microtiter plate type array(s) of reaction vessels is disclosed.