892154-56-2Relevant academic research and scientific papers
A CHIRAL RESOLUTION METHOD MIMICKING MAGNETIC BENEFICIATION AND THE MAGNETIC NANO-INHIBITORS FOR SELECTIVE ENRICHMENT
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, (2021/06/04)
A core-shell nanocomposite is formed by co-assembly of an amphiphilic polymer and hydrophobically modified magnetic nanoparticles, with its core being a hydrophobically modified magnetic nanomaterial and its shell being the amphiphilic polymer, wherein hydrophilic segments in the amphiphilic polymer are located at an outermost layer of the shell. The above composite can be used as additives in the crystallization of conglomerates and obtain optically pure crystals of both enantiomers in a single process. The key thereof is that the composite is used to enrich molecules with the same configuration while inhibit the crystallization of the other enantiomer in a supersaturated solution of conglomerates, such that a non-magnetic crystal and a magnetic crystal (which are enantiomers of each other) are generated in a unit operation. Optically pure crystals of both enantiomers with over 90 ee % can be obtained by one-time crystallization, and the total yield can be as high as 40%.
Method for preparing 1, 8 -diamino -3 and 6 -dioxaoctane through hydrogenation of triethylene glycol
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Paragraph 0024-0039, (2021/09/08)
The invention belongs to the field of fine chemical engineering, and provides a method for preparing 1, 8 -diamino -3 and 6 -dioxaoctane through hydrogen ammonification of triethylene glycol. The liquid ammonia and the secondary amine inhibitor are mixed uniformly in the storage tank according to a certain proportion, Ni / Al is injected into the plunger pump. 2 O3 A fixed bed reactor of the catalyst is subjected to ammoniation reaction under a certain process condition. Finally, the product is introduced into the gas-liquid separator to separate 1, 8 - diamino -3, 6 - dioxolane. The invention innovatively utilizes the secondary amine inhibitor and to pre-activate the catalyst to improve the reaction performance and lower the reaction pressure.
BIS(2-HALOACETAMIDO)-COMPOUNDS FOR USE AS LINKING AGENTS AND RESULTANT PRODUCTS WHICH COMPRISE ANTIBODIES, HALF-ANTIBODIES AND ANTIBODY FRAGMENTS
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, (2021/01/23)
Bis(2-haloacetamido)- compounds for use as linkers to chemically cross-linking multiple thiol groups, and particularly, although not exclusively, the thiol groups of cysteine amino acids in peptide chains are described, along with their use as linking age
Bivalent HIV-1 fusion inhibitors based on peptidomimetics
Kobayakawa, Takuya,Ebihara, Kento,Tsuji, Kohei,Kawada, Takuma,Fujino, Masayuki,Honda, Yuzuna,Ohashi, Nami,Murakami, Tsutomu,Tamamura, Hirokazu
supporting information, (2020/11/07)
Membrane fusion is a valid target for inhibition of HIV-1 replication. A 34-mer fragment peptide (C34), which is contained in the HIV-1 envelope protein gp41, has significant anti-HIV activity. Previously, a dimeric derivative of C34 linked by a disulfide bridge at its C-terminus was found to have more potent anti-HIV activity than the C34 peptide monomer. To date, several peptidomimetic small inhibitors have been reported, but most have lower potency than peptide derivatives related to C34. In the present study we applied this dimerization concept to these peptidomimetic small inhibitors and designed several bivalent peptidomimetic HIV-1 fusion inhibitors. The importance of the length of linkers crosslinking two peptidomimetic compounds was demonstrated and several potent bivalent inhibitors containing tethered peptidomimetics were produced.
Mild deprotection of the: N-tert -butyloxycarbonyl (N -Boc) group using oxalyl chloride
Awuah, Samuel G.,George, Nathaniel,Ofori, Samuel,Parkin, Sean
, p. 24017 - 24026 (2020/07/23)
We report a mild method for the selective deprotection of the N-Boc group from a structurally diverse set of compounds, encompassing aliphatic, aromatic, and heterocyclic substrates by using oxalyl chloride in methanol. The reactions take place under room temperature conditions for 1-4 h with yields up to 90percent. This mild procedure was applied to a hybrid, medicinally active compound FC1, which is a novel dual inhibitor of IDO1 and DNA Pol gamma. A broader mechanism involving the electrophilic character of oxalyl chloride is postulated for this deprotection strategy. This journal is
EXENATIDE MODIFIER AND USE THEREOF
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Paragraph 0048, (2018/05/24)
Disclosed are an exenatide modifier for connecting the exenatide to a fatty chain with a carboxy in the terminus thereof by means of a hydrophilic connecting arm, and a use thereof in preparing drugs serving as a GLP-1 receptor agonist; a use in preparing drugs for preventing and/or treating diseases and/or symptoms associated with a low GLP-1 receptor activity; a use in preparing drugs for diseases and/or symptoms associated with glycometabolism; a use in preparing drugs for diabetes; a use in preparing drugs for fatty liver disease, and a use in preparing drugs for losing weight.
Assisted enzyme replacement therapy
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Page/Page column 93; 95; 96; 97; 98, (2018/03/07)
Reagents and methods useful for the synthesis of conjugates comprising guanidinylated cyclic acetals are provided. Also provided are methods for increasing the cellular uptake of various therapeutic compounds and treatment modalities using these conjugates.
A novel graphite-like stacking structure in a discrete molecule and its molecular recognition behavior
Akine, Shigehisa,Onuma, Takahiro,Nabeshima, Tatsuya
supporting information, p. 9369 - 9372 (2018/06/18)
A graphite-like stacking structure was nicely reproduced in a discrete molecule that was prepared by 2+2 macrocyclic Schiff base formation. In the crystal structure, two hexabenzocoronene planes are closely stacked with displacement, yielding the intramolecular stacking structure similar to an AB- or ABC-stacking pattern in natural graphite. This molecule showed a recognition ability toward electron-deficient aromatic molecules in solution.
PEGylated atorvastatin derivative and preparation method thereof
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Paragraph 0050; 0052, (2018/05/03)
The invention relates to a PEGylated atorvastatin derivative and a preparation method thereof. The method mainly comprises the following steps: 1) activating an end group of PEG; 2) enabling the activated PEG to react with atorvastatin to obtain an atorvastatin analogue. The structure of the atorvastatin analogue is: Atorvastatin-L-PEG-L-Atorvastatin, wherein Atorvastatin is atorvastatin; L is anester bond, an amido bond or other linking group; the PEG is residue of monodisperse polyethylene glycol; the structural formula of the atorvastatin analogue is shown in the description, where n is aninteger between 1 and 24. The preparation method has the advantages of short flow, easiness and convenience in reaction operation, few side reactions, low cost, high reaction selectivity, easiness inpurification and higher yield.
Discovery of Macrocyclic Pyrimidines as MerTK-Specific Inhibitors
McIver, Andrew L.,Zhang, Weihe,Liu, Qingyang,Jiang, Xinpeng,Stashko, Michael A.,Nichols, James,Miley, Michael J.,Norris-Drouin, Jacqueline,Machius, Mischa,DeRyckere, Deborah,Wood, Edgar,Graham, Douglas K.,Earp, H. Shelton,Kireev, Dmitri,Frye, Stephen V.,Wang, Xiaodong
supporting information, p. 207 - 213 (2017/02/15)
Macrocycles have attracted significant attention in drug discovery recently. In fact, a few de novo designed macrocyclic kinase inhibitors are currently in clinical trials with good potency and selectivity for their intended target. In this study, we successfully engaged a structure-based drug design approach to discover macrocyclic pyrimidines as potent Mer tyrosine kinase (MerTK)-specific inhibitors. An enzyme-linked immunosorbent assay (ELISA) in 384-well format was employed to evaluate the inhibitory activity of macrocycles in a cell-based assay assessing tyrosine phosphorylation of MerTK. Through structure–activity relationship (SAR) studies, analogue 11 [UNC2541; (S)-7-amino-N-(4-fluorobenzyl)-8-oxo-2,9,16-triaza-1(2,4)-pyrimidinacyclohexadecaphane-1-carboxamide] was identified as a potent and MerTK-specific inhibitor that exhibits sub-micromolar inhibitory activity in the cell-based ELISA. In addition, an X-ray structure of MerTK protein in complex with 11 was resolved to show that these macrocycles bind in the MerTK ATP pocket.
