- Hydrosilylative reduction of primary amides to primary amines catalyzed by a terminal [Ni-OH] complex
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A terminal [Ni-OH] complex1, supported by triflamide-functionalized NHC ligands, catalyzes the hydrosilylative reduction of a range of primary amides into primary amines in good to excellent yields under base-free conditions with key functional group tolerance. Catalyst1is also effective for the reduction of a variety of tertiary and secondary amides. In contrast to literature reports, the reactivity of1towards amide reduction follows an inverse trend,i.e., 1° amide > 3° amide > 2° amide. The reaction does not follow a usual dehydration pathway.
- Bera, Jitendra K.,Pandey, Pragati
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supporting information
p. 9204 - 9207
(2021/09/20)
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- Azole derivative or pharmaceutically acceptable salt thereof as well as preparation method and application of azole derivative or pharmaceutically acceptable salt thereof
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The invention discloses an azole derivative or a pharmaceutically acceptable salt thereof and a preparation method of the azole derivative or pharmaceutically acceptable salt thereof. The structure ofthe azole derivative is as shown in the specification, and compared with the prior art, the invention provides an azole compound with a novel structure and a CRM1 protein inhibition function, and theazole compound is used as a CRM1 protein inhibitor and can block tumor cell proliferation and inhibit tumor cell apoptosis, and induce tumor cell apoptosis, and therefore, the compound can be used for treating and preventing various diseases of human and animals, such as malignant tumors, and the effect is remarkable and better.
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Paragraph 0038-0043
(2021/03/24)
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- Identifying Amidyl Radicals for Intermolecular C-H Functionalizations
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Recent studies have demonstrated the capabilities of amidyl radicals to facilitate a range of intermolecular functionalizations of unactivated, aliphatic C-H bonds. Relatively little information is known regarding the important structural and electronic features of amidyl and related radicals that impart efficient reactivity. Herein, we evaluate a diverse range of nitrogen-centered radicals in unactivated, aliphatic C-H chlorinations. These studies establish the salient features of nitrogen-centered radicals critical to these reactions in order to expedite the future development of new site-selective, intermolecular C-H functionalizations.
- Tierney, Matthew M.,Crespi, Stefano,Ravelli, Davide,Alexanian, Erik J.
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p. 12983 - 12991
(2019/10/02)
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- Synthetic process of Selinexor intermediate
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The invention provides a synthetic process of a Selinexor intermediate. The synthetic process comprises the following steps of: after inputting an intermediate 2 and -N,N'-dimethylformamide into a reaction kettle, adding sodium hydroxide; then adding magnesium chloride hexahydrate; stirring the mixture for 2-4h; adjusting the pH of a reaction system with hydrochloric acid to 1.8-2.2; performing extraction and concentration to obtain an intermediate 5; inputting the intermediate 5 and methanol into the reaction kettle; dropwise adding formylhydrazine and ethyl formate; raising the temperature to 90-95 DEG C; performing a reaction for 6-8 h; adding water after cooling; performing washing, concentration and filtration; and drying the mixture to obtain the Selinexor intermediate. According to the method, sodium hydrosulfide is not used, so that toxic gas hydrogen sulfide is no longer generated, and the synthetic process is small in environmental pollution and suitable for industrial production.
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Paragraph 0053-0061
(2017/08/29)
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- A state-of-the-art cyanation of aryl bromides: A novel and versatile copper catalyst system inspired by nature
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A general protocol for the cyanation of aryl halides with the nontoxic cyanide source K4[Fe(CN)6] using copper catalysis and a ligand system based on 1-alkylimidazoles is presented. The advantages of this system are the high selectivity, a unique substrate range, easy handling, and inexpensive reagents.
- Schareina, Thomas,Zapf, Alexander,Maegerlein, Wolfgang,Mueller, Nikolaus,Beller, Matthias
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p. 6249 - 6254
(2008/02/13)
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- 2-ARYLTHIAZOLE DERIVATIVES AS CXCR3 RECEPTOR MODULATORS
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The invention encompasses compounds of Formula I or pharmaceutically acceptable salts thereof, which are modulators of the CXCR3 chemokine receptor function useful for the treatment or prevention of pathogenic inflammatory processes, autoimmune diseases or graft rejection processes. Methods of use and pharmaceutical compositions are also encompassed.
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Page/Page column 104-105
(2010/11/28)
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- HIGH-PURITY (FLUOROALKYL)BENZENE DERIVATIVE AND PROCESS FOR PRODUCING THE SAME
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The process for producing a (fluoroalkyl)benzene derivative according to the present invention comprises a step of reducing the total content of group 3 to group 12 transition metals in an alkylbenzene derivative to 500 ppm or less in terms of metal atoms; a step of halogenating the branched alkyl group of the purified alkylbenzene derivative by a photohalogenation to obtain a (haloalkyl)benzene derivative; and a step of subjecting the (haloalkyl)benzene derivative to a halogen-fluorine exchange using HF in an amount of 10 mol or higher per one mole of the (haloalkyl)benzene derivative. The (fluoroalkyl)benzene derivative produced by the process is reduced in the content of impurities such as residual halogens and residual metals, and is useful as intermediates for functional chemical products for use in applications such as medicines and electronic materials.
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- Method of producing benzamides
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A method of producing benzamides represented by the following general formula (1): where R is trifluoromethyl group, trifluoromethyloxy group, halogen (fluorine, chlorine, bromine or iodine), nitro group, acetyl group, cyano group, alkyl group having 1 to 4 carbon atoms, alkoxy group having 1 to 4 carbon atoms, or a alkoxycarbonyl group having 2 to 5 carbon atoms; and n is 0 or an integer ranging from 1 to 3. The method comprises the step of allowing an aromatic compound represented by the following general formula (2) to react with carbon monoxide and ammonia in the presence of a metal of the group VIII of the periodic table and phosphine: where X is halogen (fluorine, chlorine, bromine or iodine), trifluoromethanesulfonate group, alkylsulfonate group having 1 to 4 carbon atoms, or substituted or unsubstituted arylsulfonate group; R is trifluoromethyl group, trifluoromethyloxy group, halogen (fluorine, chlorine, bromine or iodine), nitro group, acetyl group, cyano group, alkyl group having 1 to 4 carbon atoms, alkoxy group having 1 to 4 carbon atoms, or alkoxycarbonyl group having 2 to 5 carbon atoms; and n is 0 or an integer ranging from 1 to 3.
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