- A Facile Method for the Preparation of Nitroenamines
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Various kinds of nitroenamines are readily prepared by the reaction of 1-nitro-2-phenylthioalkenes with amines.
- Kamimura, Akio,Ono, Noboru
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- Method for synthesizing 2-amino-5-nitrothiazole
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The invention discloses a method for synthesizing 2-amino-5-nitrothiazole, which comprises the following steps: (1) in an inert atmosphere, adding diethylamine, acetyl chloride and triethyl orthoacetate into a reaction container, uniformly mixing, stirring to react for 12-24 hours, and distilling and purifying the reaction product to obtain N, N-dimethylformamide dimethyl acetal, (2) in an inert atmosphere, mixing N, N-dimethylformamide dimethyl acetal with nitromethane, heating the mixture to 80-100 DEG C for reflux reaction, carrying out reduced pressure distillation on the reaction productto remove the solvent, and purifying to obtain N, N-dimethyl nitroethylene, and (3) in an inert atmosphere, putting N, N-dimethyl nitroethylene into a reaction container, sequentially adding ethanol,liquid bromine and thiourea, reacting at room temperature, after the reaction is finished, filtering a reactant, washing with ice ethanol, drying to obtain a white solid, adding water, and filtering to obtain the 2-amino-5-nitrothiazole. According to the method for synthesizing 2-amino-5-nitrothiazole, the raw materials are easy to obtain, the cost is low, and the yield can reach 60%.
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Paragraph 0037; 0040; 0043-0050
(2020/08/06)
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- Preparation technology for 3-aryl-4-nitro isoxazole compound
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The invention discloses a preparation technology for a 3-aryl-4-nitro isoxazole compound. The preparation technology comprises the following steps: synthesizing a compound shown as formula II through the nucleophilic addition of hydroxylamine hydrochloride and the compound shown as formula I used as the raw material; acquiring the compound shown as formula III through the substitution reaction of the compound shown as formula II and N-chlorosuccinimide; preparing 1-dimethyl amino-2-nitro ethylene through the reaction of N,N-dimethylformamide dimethyl acetal and nitromethane used as the raw material; and acquiring a target product 3-aryl-4-nitro isoxazole compound through the cyclization reaction of the compound shown as formula III and 1-dimethyl amino-2-nitro ethylene. The raw materials in the synthesis route are low in cost and easily acquired, the operation condition is mild and is easily controlled, the product is easily purified and the preparation technology is a new method for synthesizing the 3-aryl-4-nitro isoxazole compound.
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Paragraph 0008; 0020; 0021; 173; 0174; 0183; 0184; 0193
(2018/03/01)
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- HETERO-HALO INHIBITORS OF HISTONE DEACETYLASE
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This invention provides compounds that are inhibitors of HDAC2. The compounds (e.g., compounds according to Formula I, II or any of Compounds 100-128 or any of those in Tables 2 or 3) accordingly are useful for treating, alleviating, or preventing a condition in a subject such as a neurological disorder, memory or cognitive function disorder or impairment, extinction learning disorder, fungal disease or infection, inflammatory disease, hematological disease, or neoplastic disease, or for improving memory or treating, alleviating, or preventing memory loss or impairment.
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Paragraph 262
(2017/01/26)
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- Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors
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Haspin is a serine/threonine kinase that phosphorylates Thr-3 of histone H3 in mitosis that has emerged as a possible cancer therapeutic target. High throughput screening of approximately 140,000 compounds identified the beta-carbolines harmine and harmol as moderately potent haspin kinase inhibitors. Based on information obtained from a structure-activity relationship study previously conducted for an acridine series of haspin inhibitors in conjunction with in silico docking using a recently disclosed crystal structure of the kinase, harmine analogs were designed that resulted in significantly increased haspin kinase inhibitory potency. The harmine derivatives also demonstrated less activity towards DYRK2 compared to the acridine series. In vitro mouse liver microsome stability and kinase profiling of a representative member of the harmine series (42, LDN-211898) are also presented.
- Cuny, Gregory D.,Ulyanova, Natalia P.,Patnaik, Debasis,Liu, Ji-Feng,Lin, Xiangjie,Auerbach, Ken,Ray, Soumya S.,Xian, Jun,Glicksman, Marcie A.,Stein, Ross L.,Higgins, Jonathan M.G.
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p. 2015 - 2019
(2012/04/05)
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- ORTHOAMIDES, XLVIII REACTIONS OF AN AZAVINYLOGUE AMINALESTER WITH CH2-ACIDIC COMPOUNDS
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Condensation reactions of azavinylogue orthoamides 5a and 6a with CH2-acidic compounds are described.Reaction products are formylated - or azavinylogue formylated compounds 8 and 9 resp.The condensation reactions of 5a can be enhanced by addition of trimethyl borate.Under these conditions the formylations reaction-leading to compounds of type 8 - is preferred.
- Kantlehner, Willi,Hauber, Michael
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p. 697 - 704
(2007/10/02)
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- 2-BENZOYLOXYNITROETHYLENE AS A CIS-2-AMINOETHENOL EQUIVALENT
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Nitroester 1 reacts readily with dienes to afford trans-nitroesters which are reduced to cis-aminoalcohols.
- Kraus, George A.,Thurston, Jeff,Thomas, P.J.,Jacobson, Robert A.,Su, Yingzhong
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p. 1879 - 1882
(2007/10/02)
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- Structural Studies on Bio-active Compounds. Part 2. The Solid-state and Solution Conformations of N-Methyl-2-nitroethenamine and Related Compounds
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The 1H n.m.r. spectra of NN-dimethyl-2-nitroethenamine, N-methyl-2-nitroethenamine, and 2-nitroethenamine in several solvents have been analysed.In the case of the monomethyl compound, the proportions of different rotamers about the C=C and C-N bonds are found to be solvent dependent.An X-ray crystallographic study of this compound indicates inter- rather than intra-molecular hydrogen bonding in the solid; molecular orbital calculations predict three of the possible four conformers about these bonds to be of similar and much lower energy than the fourth.
- Gate, E. Nicholas,Meek, Michelle A.,Schwalbe, Carl H.,Stevens, Malcolm F. G.,Threadgill, Michael D.
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p. 251 - 256
(2007/10/02)
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