- Sequential C-H activation enabled expedient delivery of polyfunctional arenes
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Modular construction of polyfunctional arenes from abundant feedstocks stands as an unremitting pursue in synthetic chemistry, accelerating the discovery of drugs and materials. Herein, using the multiple C-H activation strategy with versatile imidate esters, the expedient delivery of molecular libraries of densely functionalized sulfur-containing arenes was achieved, which enabled the concise construction of biologically active molecules, such as Bipenamol.
- Cai, Xiaoqing,Chen, Qian,Chen, Xiaojian,Gao, Yang,Huo, Yanping,Li, Xianwei,Ouyang, Wensen,Rao, Jianhang,Wang, Jie
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supporting information
p. 8075 - 8078
(2021/08/20)
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- Synthesis method of cyanoacrylate compound
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The method comprises the following reaction steps: a compound (1) reacts with a compound (2) to directly prepare a compound (3), and is characterized in that the reaction is carried out in a molten state. Compound (1). Compound (2). Compound (3).
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Paragraph 0028
(2021/09/21)
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- Synthesis of Highly Fused Pyrano[2,3- b]pyridines via Rh(III)-Catalyzed C-H Activation and Intramolecular Cascade Annulation under Room Temperature
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A facile access to the polycyclic-fused pyrano[2,3-b]pyridines has been established under room temperature via Rh(III)-catalyzed C-H bond activation and intramolecular cascade annulation. This strategy features high efficiency, unique versatility, and gen
- Han, Xu,Gao, Feng,Li, Chunpu,Fang, Daqing,Xie, Xiong,Zhou, Yu,Liu, Hong
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supporting information
p. 6281 - 6294
(2020/03/05)
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- Rh(III)-Catalyzed [3 + 2] Annulation via C-H Activation: Direct Access to Trifluoromethyl-Substituted Indenamines and Aminoindanes
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The rhodium(III)-catalyzed direct C-H addition and annulation of benzimidates and aldimines with β-(trifluoromethyl)-α,β-unsaturated ketones is described. This protocol provides the facile and efficient formation of various trifluoromethyl-containing inde
- Chaudhary, Bharatkumar,Auti, Prashant,Shinde, Suchita Dattatray,Yakkala, Prasanna Anjaneyulu,Giri, Deepesh,Sharma, Satyasheel
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supporting information
p. 2763 - 2767
(2019/04/30)
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- Rhodium-Catalyzed Relay Carbenoid Functionalization of Aromatic C-H Bonds toward Fused Heteroarenes
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A rhodium-catalyzed annulation between ethyl benzimidates and α- aroyl sulfur ylides was developed, affording a series of pyrano[4,3,2-ij]isoquinoline derivatives in moderate to good yields with good functional group compatibility. The procedure featured
- Wu, Xiaopeng,Xiong, Hao,Sun, Song,Cheng, Jiang
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supporting information
p. 1396 - 1399
(2018/03/09)
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- Controllable Rh(III)-Catalyzed C-H Arylation and Dealcoholization: Access to Biphenyl-2-carbonitriles and Biphenyl-2-carbimidates
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A controllable Rh(III)-catalyzed C-H arylation and dealcoholization of benzimidates with arylboronic esters was developed, delivering various biphenyl-2-carbonitriles and biphenyl-2-carbimidates by simply tuning the reaction conditions. This approach features high efficiency, good functional group tolerance, and easy operation. It also provides an alternative pathway to thoroughly exploit the directing group in transition-metal-catalyzed C-H activations.
- Jiang, Bo,Wu, Songxiao,Zeng, Jing,Yang, Xiaobo
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supporting information
p. 6573 - 6577
(2018/10/09)
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- Ruthenium (II)-Catalyzed Oxidant-Free Coupling/Cyclization of Benzimidates and Sulfoxonium Ylides to Form Substituted Isoquinolines
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A ruthenium-catalyzed direct mono-C?H functionalization/annulation cascade reaction of benzimidates and sulfoxonium ylides has been developed. The reaction proceeds smoothly with a broad range of substrates, giving access to a variety of isoquinoline deri
- Shi, Xinxia,Wang, Rongchao,Zeng, Xiaofei,Zhang, Yilan,Hu, Huiling,Xie, Chunsong,Wang, Min
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supporting information
p. 4049 - 4053
(2018/09/21)
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- The imine of the benzoate ester preparation method of the compound
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The invention discloses a benzimidate compound preparation method. According to the invention, a benzonitrile derivative represented by a formula (III) is subjected to a reaction with alcohol and a catalyst under a temperature of -30 DEG C to 50 DEG C, su
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Paragraph 0058; 0059
(2017/06/23)
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- Synthesis of Functionalized Indenones via Rh-Catalyzed C-H Activation Cascade Reaction
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An efficient and expeditious protocol for the synthesis of diverse difunctionalized indenones through rhodium-catalyzed C-H activation and multistep cascade reaction of benzimidates and alkenes has been developed. The transformation involves the cleavage and formation of multiple bonds in one pot under mild reaction conditions, and Mn(OAc)2 plays an important role in the reaction.
- Lv, Ningning,Chen, Zhengkai,Liu, Yue,Liu, Zhanxiang,Zhang, Yuhong
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supporting information
p. 2588 - 2591
(2017/05/24)
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- Cobalt-Catalyzed Oxidant-Free Spirocycle Synthesis by Liberation of Hydrogen
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The first example of oxidant-free cobalt-catalyzed synthesis of five-membered spirocycles is reported from benzimidates and maleimides utilizing nitrobenzene as promoter. In contrast to previously known cobalt-catalyzed oxidative C-H functionalization rea
- Lv, Ningning,Liu, Yue,Xiong, Chunhua,Liu, Zhanxiang,Zhang, Yuhong
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supporting information
p. 4640 - 4643
(2017/09/12)
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- Ruthenium(II)-Catalyzed Redox-Neutral Oxidative Cyclization of Benzimidates with Alkenes with Hydrogen Evolution
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1H-Isoindoles and 2H-isoindoles are synthesized via a ruthenium-catalyzed oxidant-free cyclization of benzimidates with alkenes at room temperature with the liberation of H2. Later, 1H-isoindoles were converted into nitrogen-containing heterocy
- Manikandan, Rajendran,Tamizmani, Masilamani,Jeganmohan, Masilamani
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supporting information
p. 6678 - 6681
(2017/12/26)
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- Synthesis of 1H-Indazoles from Imidates and Nitrosobenzenes via Synergistic Rhodium/Copper Catalysis
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Nitrosobenzenes have been used as a convenient aminating reagent for the efficient synthesis of 1H-indazoles via rhodium and copper catalyzed C-H activation and C-N/N-N coupling. The reaction occurred under redox-neutral conditions with high efficiency and functional group tolerance. Moreover, a rhodacyclic imidate complex has been identified as a key intermediate.
- Wang, Qiang,Li, Xingwei
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supporting information
p. 2102 - 2105
(2016/06/01)
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- Rh(III)-Catalyzed C-C/C-N Coupling of Imidates with α-Diazo Imidamide: Synthesis of Isoquinoline-Fused Indoles
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Imidate esters and diazo compounds have been established as bifunctional substrates for the construction of biologically active fused heterocycles via rhodium-catalyzed C-H activation and C-C/C-N coupling. This reaction occurs under mild conditions with high efficiency, step economy, and low catalyst loading.
- Wang, He,Li, Lei,Yu, Songjie,Li, Yunyun,Li, Xingwei
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supporting information
p. 2914 - 2917
(2016/07/06)
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- Convenient synthesis of 5-substituted 2-amino[1,2,4]triazolo[1,5- a ][1,3,5]triazin-7(6 H)-ones from N -triazolide imidates and 1,2,4-Triazole-3,5- diamine
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A convenient and efficient synthesis of previously unreported N-triazolide imidates and their reaction with 1,2,4-triazole-3,5-diamine to give regioselectively 5-substituted 2-amino[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(6H) -ones is described. The structure of the reported bicyclic compounds has been unambiguously proven by X-ray crystallography. Georg Thieme Verlag Stuttgart.
- Khankischpur, Mehdi,Hansen, Finn K.,Geffken, Detlef
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experimental part
p. 1645 - 1648
(2010/06/19)
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- Processes For The Preparation Of Anti-Viral Compounds And Compositions Containing Them
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Disclosed are processes for the preparation of compounds of formula I and compositions that comprise said compounds of formula I. Also disclosed are processes for the preparation of compounds of formula III and compositions that comprise said compounds of formula III.
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Page/Page column 83
(2010/03/02)
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- ANTI-VIRAL COMPOUNDS, COMPOSITIONS, AND METHODS OF USE
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Disclosed are compounds of Formula (I), pharmaceutically acceptable salts and solvates thereof, compositions thereof, and methods for their preparation and uses for treating viral infections mediated at least in part by a virus in the Flaviviridae family of viruses. (I)
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Page/Page column 103
(2009/03/07)
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- PYRIDYL AND PHENYL SUBSTITUTED PIPERAZINE-PIPERIDINES WITH CXCR3 ANTAGONIST ACTIVITY
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The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates and esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non limiting example(s) include, psoriasis), autoimmune diseases (non limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g , tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
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Page/Page column 146
(2008/06/13)
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- Total synthesis of the thiopeptide antibiotic amythiamicin D
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The thiopeptide (or thiostrepton) antibiotics are a class of sulfur containing highly modified cyclic peptides with interesting biological properties, including reported activity against MRSA and malaria. Described herein is the total synthesis of the thi
- Hughes, Rachael A.,Thompson, Stewart P.,Alcaraz, Lilian,Moody, Christopher J.
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p. 15644 - 15651
(2007/10/03)
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- A remarkably efficient Markovnikov hydrochlorination of olefins and transformation of nitriles into imidates by use of AcCl and an alcohol
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HCl generated by mixing AcCl with EtOH brings about Markovnikov hydrochlorination of olefins in excellent yields. The products are isolated in states of high purity simply by removal of the volatile components under reduced pressure. Further, nitriles are transformed into imidate hydrochlorides on similar treatment with AcCl and an alcohol. This procedure for nitrile-imidate transformation is much more efficient than that used previously, which involved continuous passing of HCl gas into the solution of a nitrile in a solvent such as Et2O or benzene and an alcohol until one equivalent had been absorbed. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2005.
- Yadav, Veejendra K.,Babu, K. Ganesh
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p. 452 - 456
(2007/10/03)
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- The conversion of amides to esters with Meerwein's reagent. Application to the synthesis of a carfentanil precursor
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An efficient two step transformation of 1°and 2°amides to methyl and ethyl esters has been developed using trimethyl- and triethyloxonium tetrafluoroborates, and dilute acid. This methodology was applied to 1-benzyl-4-phenylamino-4-piperidinecarboxamide, a precursor in the synthesis of carfentanil, to produce the methyl ester in 60% yield and the ethyl ester in 80% yield.
- Kiessling, Anthony J.,McClure, Cynthia K.
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p. 923 - 937
(2007/10/03)
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- SYNTHESE ET REACTIVITE D'ARYL ET ALKYL-2 (4H) PYRIDO THIAZINE-1,3 ONES-4
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2-Aryl and alkyl pyrido -1,3-thiazine-4(4H)-ones, a class of previously unknown compounds can be conveniently prepared by treatment of the sodium anion of 2-chloronicotinamide with various aromatic and aliphatic thioesters.Their reduction with sodi
- Couture, Axel,Grandclaudn, Pierre,Huguerre, Eric
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p. 4153 - 4162
(2007/10/02)
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- A Facile and Concise Synthesis of 2-Alkyl- and 2-Aryl-4-oxo-4H-thiopyranopyridines
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2-Alkyl- and 2-aryl-4-oxo-4H-thiopyranopyridine can be conveniently prepared by reacting the appropriate aromatic and aliphatic O-ethyl thiocarboxylates with the sodium derivative of various alkyl 3-(2-bromopyridyl) ketones.
- Couture, Axel,Grandclaudon, Pierre,Huguerre, Eric
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p. 456 - 457
(2007/10/02)
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