929-59-9Relevant articles and documents
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.
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
PEGylated atorvastatin derivative and preparation method thereof
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Paragraph 0046; 0048, (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.
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.
Preparation method of 2-(2-(2-amidogen ethyoxyl) ethyoxyl) ethyl carbamic acid tert-butyl ester
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Paragraph 0043; 0044; 0047, (2017/08/29)
The invention relates to a preparation method of a 2-(2-(2-amidogen ethyoxyl) ethyoxyl) ethyl carbamic acid tert-butyl ester. The method comprises the following steps of reacting ethylene glycol and haloacetonitrile at the temperature of 0 to 60 DEG C under the existence of alkali, and obtaining 1,6-dicyano-2,5-dioxa hexane in a formula (I); carrying out reduction reaction on the 1,6-dicyano-2,5-dioxa hexane in the formula (I) in an organic solvent, and obtaining 1,8-diamido-3,6-dioxa octane in a formula (II); carrying out Boc monoprotection reaction on the 1,8-diamido-3,6-dioxa octane in the formula (II) and a di-tert-butyl dicarbonate ester in an organic solvent, and obtaining the 2-(2-(2-amidogen ethyoxyl) ethyoxyl) ethyl carbamic acid tert-butyl ester in a formula (III), wherein a reaction route is as shown in the below figure, and X is chlorine, bromine or iodine. The preparation method provided by the invention is less in operation steps and simple and convenient, not only can overcome the defect that the 1,8-diamido-3,6-dioxa octane obtained through a traditional Staudinger reduction method contains water, but also can avoid the insecurity of azide, and is suitable for industrial production.
Tetracyclic benzimidazole derivatives and combinatorial libraries thereof
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, (2008/06/13)
The present invention relates to novel tetracyclic benzimidazole derivative compounds of the following formula: wherein R1to R10have the meanings described in here. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing tetracyclic benzimidazole derivative compounds.
Anti-malarial activity of N6-substituted adenosine derivatives. Part I
Golisade, Abolfasl,Wiesner, Jochen,Herforth, Claudia,Jomaa, Hassan,Link, Andreas
, p. 769 - 777 (2007/10/03)
The synthesis and biological evaluation of novel N6-substituted adenosine derivatives is reported. The first series of compounds was obtained using an established procedure for the nucleophilic substitution of a 1-(6-chloro-purin-9-yl)-β-D-1-deoxy-ribofuranose with various amines. In addition, attachment of two different amino-functionalised spacer arms at the N6-position of adenosine enabled derivatisation by an innovative polymer-assisted protocol. Thus, we were able to prepare three series of substituted derivatives that displayed activity versus the multiresistant Plasmodium falciparum strain Dd2 in cell culture experiments.
Neoglycoproteins
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, (2008/06/13)
Polyamide conjugates comprising either (a) a xenoantigenic group; or (b) a biologically active group and a macromolecular, macro- or microscopic entity, bound to a polyamide backbone, processes for their preparation and the use of these conjugates in therapeutic compositions.
Diamine platinum naphthalimide complexes as antitumor agents
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, (2008/06/13)
The present invention provides novel bis-naphthalimides characterized by having a linker containing a heteroatom, their preparation, pharmaceutical compositions thereof, and various methods of using the bis-naphthalimides. Particularly preferred bis-naphthalimides have a linker of about 8-16 atoms where the heteroatom is oxygen, sulfur, sulfur oxide or sulfur dioxide. The bis-naphthalimides provided herein have exceptional DNA binding properties and demonstrate cytotoxicity in both in vitro and in vivo tumor models, in particular, against melanoma. Also provided a novel mono-naphthalimides linked to a DNA alkylating agent. These agents are shown to have conformational effects on double stranded DNA and to form covalent adducts after an extended incubation period.