- Supramolecular compound nano-carrier as well as preparation method and application thereof
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The invention discloses a supramolecular compound nano-carrier as well as a preparation method and application thereof, and relates to the technical field of polymer chemistry and biological detection engineering. According to the supramolecular compound nano-carrier disclosed by the invention, a two-dimensional nanosheet supramolecular structure system generated by self-assembly is driven by an anion induction effect, and a supramolecular compound nano-carrier is of a single-layer nanosheet supramolecular structure constructed by a highly-oriented one-dimensional nanorod. A hydrophobic perylene group part is used as a skeleton part for constructing the highly-oriented one-dimensional nanorod, and the charge density of a single-layer nanosheet can be regulated and controlled. The surface of the water-soluble multivalent hydrophilic part can be loaded with DNAzyme deoxyribozyme for specific detection of heavy metal ions through electrostatic interaction, and the water-soluble multivalent supramolecular compound nano sensor is constructed. Based on a fluorescence change mechanism caused by specific cutting of heavy metal ions, The fluorescence detection of the heavy metal ions in food and biological tissues is realized, and the detection effect of the heavy metal ions is greatly enhanced.
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Paragraph 0104-0108
(2021/08/14)
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- PROTAC compound for targeted degradation of IDO1, and preparation method and application thereof
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The invention provides a PROTAC compound represented by formula I and used for targeted degradation of IDO1, and a pharmaceutically acceptable salt, a hydrate or a solvate thereof. In the formula I, Xrepresents -CH2 or -C = O, Y represents -CH2 or -C= O, and n is a natural number from 2 to 9. The PROTAC compound for targeted degradation of the IDO1 has efficient activity of targeted degradation of the IDO1 protein.
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Paragraph 0024-0026; 0036-0037
(2020/06/17)
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- Optimization of IEDDA bioorthogonal system: Efficient process to improve trans-cyclooctene/tetrazine interaction
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The antibody pretargeting approach for radioimmunotherapy (RIT) using inverse electron demand Diels-Alder cycloaddition (IEDDA) constitutes an emerging theranostic approach for solid cancers. However, IEDDA pretargeting has not reached clinical trial. The major limitation of the IEDDA strategy depends largely on trans-cyclooctene (TCO) stability. Indeed, TCO may isomerize into the more stable but unreactive cis-cyclooctene (CCO), leading to a drastic decrease of IEDDA efficiency. We have thus developed both efficient and reproducible synthetic pathways and analytical follow up for (PEGylated) TCO derivatives, providing high TCO isomeric purity for antibody modification. We have set up an original process to limit the isomerization of TCO to CCO before the mAbs’ functionalization to allow high TCO/tetrazine cycloaddition.
- Béquignat, Jean-Baptiste,Boucheix, Claude,Canitrot, Damien,Chezal, Jean-Michel,Degoul, Fran?oise,Miot-Noirault, Elisabeth,Moreau, Emmanuel,Navarro-Teulon, Isabelle,Quintana, Mercedes,Rondon, Aurélie,Taiariol, Ludivine,Ty, Nancy
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supporting information
(2020/07/21)
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- Highly efficient synthesis of monodisperse poly(ethylene glycols) and derivatives through macrocyclization of oligo(ethylene glycols)
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A macrocyclic sulfate (MCS)-based approach to monodisperse poly(ethylene glycols) (M-PEGs) and their monofunctionalized derivatives has been developed. Macrocyclization of oligo(ethylene glycols) (OEGs) provides MCS (up to a 62-membered macrocycle) as versatile precursors for a range of monofunctionalized M-PEGs. Through iterative nucleophilic ring-opening reactions of MCS without performing group protection and activation, a series of M-PEGs, including the unprecedented 64-mer (2850Da), can be readily prepared. Synthetic simplicity coupled with versatility of this new strategy may pave the way for broader applications of M-PEGs. Macrocycles make synthesis easier: Convenient macrocyclization of the OEGs provides versatile macrocyclic sulfates. These compounds are cornerstones for both monofunctionalization of OEGs and highly efficient synthesis of monodisperse PEGs and derivatives, including an unprecedented 64-mer.
- Zhang, Hua,Li, Xuefei,Shi, Qiuyan,Li, Yu,Xia, Guiquan,Chen, Long,Yang, Zhigang,Jiang, Zhong-Xing
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p. 3763 - 3767
(2015/03/18)
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- Convenient multigram synthesis of monodisperse oligo(ethylene glycols): Effective reaction monitoring by infrared spectroscopy using an attenuated total reflection fibre optic probe
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A convenient approach for the synthesis of monodisperse oligo(ethylene glycols) up to 12 units is described. A novel cleavage protocol replacing laborious hydrogenolysis is introduced to achieve a fast, inexpensive and widely applicable procedure. In addition to the synthetic part, Fourier transform infrared (FTIR) spectroscopy using a fibre optic attenuated total reflection (ATR) sensor was applied to monitor the formation of sensitive key intermediates, resulting in optimized reaction times. By applying this in-line technique, the possibility of real-time analysis under inert conditions was impressively demonstrated.
- Lumpi, Daniel,Braunshier, Christian,Hametner, Christian,Horkel, Ernst,Zachhuber, Bernhard,Lendl, Bernhard,Fr?hlich, Johannes
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supporting information; experimental part
p. 6469 - 6471
(2011/02/23)
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- Synthesis of oligo(ethylene glycol) toward 44-mer
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A synthetic method for oligo(ethylene glycol) toward 44-mer (FW = 1956.35) is described. Reiteration of Williamson's ether synthesis and hydrogenation to remove protecting benzyl group affords desired oligo(ethylene glycol) toward 44-mer in moderate yields. The advantages in this method are use of commercially easily available materials as starting materials and procedures avoiding difficulty in purification of the products as much as possible.
- Ahmed, Saleh A.,Tanaka, Mutsuo
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p. 9884 - 9886
(2007/10/03)
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- An expedient synthesis of monodispersed oligo(ethylene glycols)
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A convenient approach to the synthesis of oligo(ethylene glycols) under phase transfer conditions is described. Oligo(ethylene glycols) (x = 7-12) are obtained in excellent yields and high purity via modular, bi-directional elongation of readily available ethylene glycol bis-tosylates.
- Burkett, Brendan A.,Chan, Tak Hang
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p. 1007 - 1010
(2007/10/03)
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- HIV protease inhibitors having polyether substituents
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[From equivalent EP0487270A2] Polyether derivatives of the form, A-G-B-B-J ψ wherein G is a dipeptide isostere substituted with a polyether, B an amino acid or analog thereof, and J a small terminal group are described. These compounds are useful in the inhibition of DIV protease, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.ψ
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- Intramolecular End-to-End Reactions of Photoactive Terminal Groups Linked by Poly(oxyethylene) Chains
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The triplet-sensitized photochemical reaction using a series of poly(oxyethylene) chains with a pair of photoactive terminal groups, dibenzazepine (DBA) chromophores (DBA-COCH2CH2(OCH2CH2)nOCH2CH2CO-DBA, n=0-10) was examined.The photoirradiation of bichromophoric compounds caused either intra- or intermolecular reactions.These reactions were kinetically analyzed by two different methods: the measurement of deactivation processes of the reaction intermediates (excited triplet state of DBA) by nanosecond laser photolysis and the quantitative analysis of the reaction products by GPC.The intramolecular deactivation rate constant, kintra, showed a remarkable chain-length dependence; the maximum kintra value appeared at n=5 and it was found to be 5.9X104 s-1.On the other hand, the intramolecular cyclization rate also depends on the chain length; the maximum quantum yield, φintrad, was given at n=7 (φintrad=0.51).The chain length for the maximum cyclization yield shifted slightly to the longer region than that for the maximum kintra value due to the restriction of the terminal structure (anti-configuration).The results obtained for this reaction system are compared with those obtained for the previously reported polymethylene system and the effect of chain flexibility on the intramolecular ring-closure reaction is discussed.
- Ashikaga, Kazuo,Ito, Shinzaburo,Yamamoto, Masahide,Nishijima, Yasunori
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p. 2443 - 2450
(2007/10/02)
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- A Facile Synthesis of Hexa- and Octaethylene Glycols
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One-pot syntheses of hexa- and octaethylene glycol are achieved by the reaction of tri- or tetraethylene glycol with tosyl chloride in the presence of an appropriate base followed by a Williamson-type condensation reaction.
- Nakatsuji, Yohji,Kameda, Nobuko,Okahara, Mitsuo
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p. 280 - 281
(2007/10/02)
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- A NOVEL, UNEQUIVOCAL SYNTHESIS OF POLYETHYLENE GLYCOLS
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Unequivocal synthesis of polyethyleneglycols is presented.The key step for this synthesis is the selective monobenzylation of oligoethyleneglycols by the phase transfer catalysis technique.
- Coudert, Gerard,Mpassi, Michel,Guillaumet, Gerald,Selve, Claude
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- The Influence of Cation Binding on the Kinetics of the Hydrolysis of Crown Ether Acetals
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The rate of hydrogen ion-catalysed hydrolysis of crown ether acetals in 60:40 (v/v) dioxan-water is found to be strongly decreased by the addition of alkali and alkaline earth metal chlorides having cations of appropriate size to be complexed by the substrate ring.The compounds studied are the monoacetals CH3CH(OCH2CH2)xO with x=1-8.The dependence of the initial rate of formation of acetaldehyde on metal-ion concentration is expressed in terms of (i) the equilibrium constant for complex formation, (ii) the influence of the bound cation on the rate constant, and (iii) an electrolyte effect.A curve-fitting procedure is used to derive the parameters governing the first two of these effects.The equilibrium constants are large and cannot be evaluated with any precision, but a fair estimate of the influence of the guest cation on the rate can be obtained.This effect is explicable by the electrostatic repulsion between the cationic charges of the metal ion and the proton added to the acetal in the first step of the hydrolysis.The size of the effect requires the values of the effective relative permittivity of the space between the charges to be close to that of the bulk solvent.
- Baker, David S.,Gold, Victor,Sghibartz, Cristian M.
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p. 1121 - 1128
(2007/10/02)
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