- Synthesis of CF3CH2-Containing Indolines by Transition-Metal-Free Aryltrifluoromethylation of Unactivated Alkenes
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With an unactivated double bond as the radical acceptor, allyl amines underwent a metal-free trifluoromethylation/cyclization cascade with CF3SO2Na (Langlois' reagent), affording CF3CH2-containing indolines and tetrahydroisoquinolines, whose practical syntheses are significant challenges. This protocol features mild conditions, low cost, and a broad substrate scope.
- Liang, Deqiang,Dong, Qishan,Xu, Penghui,Dong, Ying,Li, Weili,Ma, Yinhai
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p. 11978 - 11986
(2018/09/27)
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- Synthetic method of CF3-containing indoline and 1,2,3,4-tetrahydroisoquinoline
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The invention discloses a synthetic method of CF3-containing indoline and 1,2,3,4-tetrahydroisoquinoline and relates to the technical field of compound synthesis. The synthetic method herein is basedon metal-free trifluoromethylation/cyclization free radical cascade reaction using a nonactive olefin dual-bond as a free radical receptor; the reaction aforementioned helps synthesize, in one step, CF3-containing indoline and 1,2,3,4-tetrahydroisoquinoline. The synthetic method herein has the significant advantages of mild conditions, good operational simplicity, low cost, wide substrate range, good exo selectivity and the like.
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Paragraph 0027; 0029; 0030; 0031; 0042
(2019/01/14)
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- N - substituted benzyl amino phosphine pliers link ruthenium double phosphine compound and its preparation method and application
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The invention relates to an N-substituted benzylaminophosphonic pincer-type cyclo-ruthenium diphosphonic compound, and a preparation method and an application for the N-substituted benzylaminophosphonic pincer-type cyclo-ruthenium diphosphonic compound. The preparation method comprises the following steps of adding amine phosphine, substituted benzyl alcohol, diphosphine ligand, RuC12(PPh3)3 and alkali into organic solvent; heating the mixture under the protection of N2 gas; filtering and recrystallizing the mixture so as to obtain the N-substituted benzylaminophosphonic pincer-type cyclo-ruthenium diphosphonic compound after the reaction is completed, wherein the process of synthesizing the N-substituted benzylaminophosphonic pincer-type cyclo-ruthenium diphosphonic compound is eliminated, so that the reaction operation is simple, and the preparation is easy. According to the preparation method, the N-substituted benzylaminophosphonic pincer-type cyclo-ruthenium diphosphonic compound is taken as a metal catalyst for catalytically synthesizing and preparing amide compounds. The preparation method has the advantages of low price and wide range of reaction substrates, mild condition, high efficiency and practicability, and has important application values.
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Paragraph 0070; 0071
(2017/10/07)
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- INHIBITORS OF FATTY ACID AMIDE HYDROLASE
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The present invention provides compounds, and pharmaceutically acceptable compositions thereof, encompassed by any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof. The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof.
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Paragraph 1036
(2016/01/15)
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- Ligand-enabled triple C-H activation reactions: One-pot synthesis of diverse 4-aryl-2-quinolinones from propionamides
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Diverse 4-aryl-2-quinolinones are prepared from propionamides in one pot by ligand-promoted triple sequential C-H activation reactions and a stereospecific Heck reaction. In these cascade reactions, three new C-C bonds and one C-N bond are formed to rapidly build molecular complexity from propionic acid. Building complexity: Diverse 4-aryl-2-quinolinones such as 1 are prepared from propionamides in one pot by pyridine ligand-promoted triple sequential C-H activation reactions and a stereospecific Heck reaction. In these cascade reactions, three new C-C bonds and one C-N bond are formed to rapidly build molecular complexity from propionic acid.
- Deng, Youqian,Gong, Wei,He, Jian,Yu, Jin-Quan
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supporting information
p. 6692 - 6695
(2014/07/08)
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- Discovery and structure-activity relationship of potent and selective covalent inhibitors of transglutaminase 2 for Huntington's disease
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Tissue transglutaminase 2 (TG2) is a multifunctional protein primarily known for its calcium-dependent enzymatic protein cross-linking activity via isopeptide bond formation between glutamine and lysine residues. TG2 overexpression and activity have been found to be associated with Huntington's disease (HD); specifically, TG2 is up-regulated in the brains of HD patients and in animal models of the disease. Interestingly, genetic deletion of TG2 in two different HD mouse models, R6/1 and R6/2, results in improved phenotypes including a reduction in neuronal death and prolonged survival. Starting with phenylacrylamide screening hit 7d, we describe the SAR of this series leading to potent and selective TG2 inhibitors. The suitability of the compounds as in vitro tools to elucidate the biology of TG2 was demonstrated through mode of inhibition studies, characterization of druglike properties, and inhibition profiles in a cell lysate assay.
- Prime, Michael E.,Andersen, Ole A.,Barker, John J.,Brooks, Mark A.,Cheng, Robert K. Y.,Toogood-Johnson, Ian,Courtney, Stephen M.,Brookfield, Frederick A.,Yarnold, Christopher J.,Marston, Richard W.,Johnson, Peter D.,Johnsen, Siw F.,Palfrey, Jordan J.,Vaidya, Darshan,Erfan, Sayeh,Ichihara, Osamu,Felicetti, Brunella,Palan, Shilpa,Pedret-Dunn, Anna,Schaertl, Sabine,Sternberger, Ina,Ebneth, Andreas,Scheel, Andreas,Winkler, Dirk,Toledo-Sherman, Leticia,Beconi, Maria,MacDonald, Douglas,Mu?oz-Sanjuan, Ignacio,Dominguez, Celia,Wityak, John
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p. 1021 - 1046
(2012/04/10)
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- Synthesis and supramolecular self-assembly of coil-rod-coil molecules: The relationship between self-assembled nanostructures and molecular structures
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Herein, the relationship between the supramolecularly self-assembled nanostructures and the chemical structures of coil-rod-coil molecules is discussed. A series of nonamphiphilic coil-rod-coil molecules with different alkyl chains, central mesogenic grou
- Chen, Yulan,Zhang, Fan,Zhu, Bo,Han, Yang,Bo, Zhishan
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experimental part
p. 226 - 233
(2011/09/16)
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- An efficient protocol for the amidation of carboxylic acids promoted by trimethyl phosphite and iodine
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A practical, one-pot protocol is described for the conversion of carboxylic acids into amides through carboxyl activation by the reagent combination of trimethyl phosphite and iodine. This method integrates several advantages: (1) it allows amines to be chemoselectively acylated with excellent results in the presence of sulfur and oxygen nucleophiles; (2) the method shows wide generality in respect of solvent, base, and substrate; (3) the reagents used are widely available and much less expensive than common coupling reagents, and (4) the process is remarkably convenient, permitting extraction, recrystallization, and column chromatography as optional work-up procedures. The chemoselectivity and generality of the method, the low cost, and wide availability of reagents combined with the ease of use make it a very favorable process.
- Luo, Qun-Li,Lv, Lina,Li, Yu,Tan, Jian-Ping,Nan, Wenhui,Hui, Qun
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supporting information; experimental part
p. 6916 - 6922
(2012/01/06)
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- METHOD OF PROCESSING OF HYDROGEN FOR REDUCTIVE ACYLATION OF NITRO, AZIDO AND CYANO ARENES
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The present invention relates to a method for processing of hydrogen for the reductive acylation of nitro, azido and cyano arenes. More particularly, this invention relates to an improved process for the preparation of amides and anilides using C3-C7 carboxylic acids as proton source/acylating agents employing Fe3+-montmorillonite as a catalyst.
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- Method of processing of hydrogen for reductive acylation of nitro, azido and cyano arenes
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A method for processing of hydrogen for the reductive acylation of nitro, azido and cyano arenes is disclosed. More particularly, improved process for the preparation of amides and anilides using C3-C7carboxylic acids as proton source/acylating agents employing Fe3+-montmorillonite as a catalyst is disclosed.
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Page column 5
(2008/06/13)
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- Solid phase synthesis of amides by the Beckmann rearrangement of ketoxime carbonates
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In the presence of trifluoroacetic acid, ketoxime benzyl carbonates undergo a Beckmann rearrangement to the corresponding amides. This reaction was translated to a solid support by immobilizing oximes in the form of mixed carbonates derived from hydroxymethylpolystyrene in order to produce a diversity of amides with high efficiency.
- His, Sarah,Meyer, Christophe,Cossy, Janine,Emeric, Gibert,Greiner, Alfred
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p. 8581 - 8584
(2007/10/03)
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