86386-65-4Relevant academic research and scientific papers
Preparation method of N-(aryl/heteroaryl) alkyl-diamide
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Paragraph 0029-0030, (2020/12/29)
The invention relates to a preparation method of N-(aryl/heteroaryl)alkyl- diamide, which comprises the following steps: under the protection of nitrogen, sequentially adding transition metal, phosphine or nitrogen ligand, cocatalyst, alkali, solvent, Nhalogenated cyclodiamide, alkyl aromatic ring or alkyl heteroaromatic ring compound into a reaction container, carrying out oxidative amination reaction at 80-140 DEG C, and till the reaction concludes after 6-48 hours, evaporating and drying a solvent and carrying out column chromatography separation to obtain an N (aryl/heteroaryl) alkyl diamide compound. The invention is simple in synthesis process, mild in reaction condition, high in yield and easy to industrialize.
MANGANESE BASED COMPLEXES AND USES THEREOF FOR HOMOGENEOUS CATALYSIS
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Paragraph 00394, (2017/09/05)
The present invention relates to novel manganese complexes and their use, inter alia, for homogeneous catalysis in (1) the preparation of imine by dehydrogenative coupling of an alcohol and amine; (2) C-C coupling in Michael addition reaction using nitriles as Michael donors; (3) dehydrogenative coupling of alcohols to give esters and hydrogen gas (4) hydrogenation of esters to form alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di- lactones), or polyesters); (5) hydrogenation of amides (including cyclic dipeptides, lactams, diamide, polypeptides and polyamides) to alcohols and amines (or diamine); (6) hydrogenation of organic carbonates (including polycarbonates) to alcohols or hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (7) dehydrogenation of secondary alcohols to ketones; (8) amidation of esters (i.e., synthesis of amides from esters and amines); (9) acylation of alcohols using esters; (10) coupling of alcohols with water and a base to form carboxylic acids; and (11) preparation of amino acids or their salts by coupling of amino alcohols with water and a base. (12) preparation of amides (including formamides, cyclic dipeptides, diamide, lactams, polypeptides and polyamides) by dehydrogenative coupling of alcohols and amines; (13) preparation of imides from diols.
Synthesis of Cyclic Imides by Acceptorless Dehydrogenative Coupling of Diols and Amines Catalyzed by a Manganese Pincer Complex
Espinosa-Jalapa, Noel Angel,Kumar, Amit,Leitus, Gregory,Diskin-Posner, Yael,Milstein, David
supporting information, p. 11722 - 11725 (2017/09/07)
The first example of base-metal-catalyzed dehydrogenative coupling of diols and amines to form cyclic imides is reported. The reaction is catalyzed by a pincer complex of the earth abundant manganese and forms hydrogen gas as the sole byproduct, making the overall process atom economical and environmentally benign.
Structure-based design of phthalimide derivatives as potential cyclooxygenase-2 (COX-2) inhibitors: Anti-inflammatory and analgesic activities
Alanazi, Amer M.,El-Azab, Adel S.,Al-Suwaidan, Ibrahim A.,Eltahir, Kamal Eldin H.,Asiri, Yousif A.,Abdel-Aziz, Naglaa I.,Abdel-Aziz, Alaa A.-M.
, p. 115 - 123 (2015/02/19)
A group of 30 cyclic imides (1-10a-c) was designed for evaluation as a selective COX-2 inhibitor and investigated in vivo for anti-inflammatory and analgesic activities. Compounds 6a, 6b, 7a and 7b exhibit optimal COX-2 inhibitory potency (IC50 Combining double low line 0.18, 0.24, 0.28 and 0.36 μM; respectively) and selectivity index (SI) range of 363-668. In vitro COX-1/COX-2 inhibition structure-activity studies identified compound 6a as a highly potent (IC50 Combining double low line 0.18 μM), and an extremely selective [COX-2 (SI) Combining double low line 668] comparable to celecoxib [COX-2 (SI) > 384], COX-2 inhibitor that showed superior anti-inflammatory activity (ED50 Combining double low line 54.0 mg/kg) relative to diclofenac (ED50 Combining double low line 114 mg/kg). Molecular Docking study of the synthesized compound 6a into the active site of COX-2 revealed a similar binding mode to SC-558, a selective COX-2 inhibitor. Docking study showed that the methoxy moeities of 6a inserted deep inside the 2°-pocket of the COX-2 active site, where the O-atoms of such groups underwent an H-bonding interaction with His90 (3.02 g.,), Arg513 (1.94, 2.83 g.,), and Gln192 (3.25 g.,).
Porous material-immobilized iodo-Bodipy as an efficient photocatalyst for photoredox catalytic organic reaction to prepare pyrrolo[2,1-a]isoquinoline
Guo, Song,Zhang, Hongli,Huang, Ling,Guo, Zhendong,Xiong, Guang,Zhao, Jianzhang
supporting information, p. 8689 - 8691 (2013/09/23)
Iodo-Bodipy immobilized on porous silica was used as an efficient recyclable photocatalyst for photoredox catalytic tandem oxidation-[3+2] cycloaddition reactions of tetrahydroisoquinoline with N-phenylmaleimides to prepare pyrrolo[2,1-a]isoquinoline.
PROCESS OF FORMING A CYCLIC IMIDE
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Page/Page column 30, (2012/01/15)
A process is provided for the synthesis of a cyclic imide. A primary amine and a diol compound are contacted in the presence of a Ruthenium (II) complex. The Ruthenium (II) catalyst includes at least one of an alicyclic ligand, an aromatic ligand, an arylalicyclic ligand, an arylaliphatic ligand and a phosphine ligand.
Synthesis of cyclic imides from simple diols
Zhang, Jian,Senthilkumar, Muthaiah,Ghosh, Subhash Chandra,Hong, Soon Hyeok
supporting information; experimental part, p. 6391 - 6395 (2010/11/05)
There's something imide so strong: Cyclic imides were synthesized from simple diols with primary amines in a single step using an in-situ-generated ruthenium catalytic system. The atom-economical and operatively simple syntheses of succinimides, phthalimides, and glutarimides, which are important building blocks in natural products and drugs, was also demonstrated. Copyright
Processes and intermediates useful for preparing integrase inhibitor compounds
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Page/Page column 16-17, (2010/11/30)
The invention provides processes and intermediates useful for preparing integrase inhibiting compounds.
Integrase inhibitor compounds
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Page/Page column 58, (2010/11/26)
Tricyclic compounds, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.
Design and optimization of tricyclic phtalimide analogues as novel inhibitors of HIV-1 integrase
Verschueren, Wim G.,Dierynck, Inge,Amssoms, Katie I. E.,Hu, Lili,Boonants, Paul M. J. G.,Pille, Geert M. E.,Daeyaert, Frits F. D.,Hertogs, Kurt,Surleraux, Dominique L. N. G.,Wigerinck, Piet B. T. P.
, p. 1930 - 1940 (2007/10/03)
Human immunodeficiency virus type-1 integrase is an essential enzyme for effective viral replication and hence a valid target for the design of inhibitors. We report here on the design and synthesis of a novel series of phthalimide analogues as integrase
