- Method for preparing N-sulfonyl tetrahydropyrrole compound by using gold complex
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The invention relates to a method for preparing an N-sulfonyl tetrahydropyrrole compound by using a gold complex, which comprises the following step of: reacting a sulfonamide compound and a tetrahydrofuran compound as raw materials with a gold complex containing an ortho-carborane Schiff base ligand as a catalyst at room temperature to obtain the N-sulfonyl tetrahydropyrrole compound. Compared with the prior art, the method has the advantages that the gold complex containing the ortho-carborane Schiff base ligand is adopted as the catalyst, the sulfonamide compound and the tetrahydrofuran compound can be catalyzed to react under the room temperature condition to prepare the N-sulfonyl tetrahydropyrrole compound, the usage amount of the catalyst is low, the reaction condition is mild, the reaction rate is high, the product yield is high, the substrate is high in universality, the raw materials are cheap and easy to obtain, and the method has a wide application prospect in industry.
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Paragraph 0054-0059
(2021/07/17)
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- Optimization of norbornyl-based carbocyclic nucleoside analogs as cyclin-dependent kinase 2 inhibitors
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We report on the discovery of norbornyl moiety as a novel structural motif for cyclin-dependent kinase 2 (CDK2) inhibitors which was identified by screening a carbocyclic nucleoside analogue library. Three micromolar hits were expanded by the use of medic
- K?prülüo?lu, Cemal,Dejmek, Milan,?ála, Michal,Ajani, Haresh,H?ebabecky, Hubert,Fanfrlík, Jind?ich,Jorda, Radek,Dra?ínsky, Martin,Procházková, Eli?ka,?ácha, Pavel,Kry?tof, Vladimír,Hobza, Pavel,Lep?ík, Martin,Nencka, Radim
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- Iodine-catalyzed sulfonylation of sulfonyl hydrazides with: Tert -amines: A green and efficient protocol for the synthesis of sulfonamides
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This study provides a direct, sustainable and eco-friendly method for the synthesis of various sulfonamides via the sulfonylation of sulfonyl hydrazides with tert-amines. The method utilizes sulfonyl hydrazides to oxidize and couple with tertiary amines through selective cleavage of C-N bonds. In this reaction, molecular iodine was used as the catalyst and t-butyl hydroperoxide was used as the oxidant.
- Chen, Jinyang,Han, Xiaoran,Mei, Lan,Liu, Jinchuan,Du, Kui,Cao, Tuanwu,Li, Qiang
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p. 31212 - 31216
(2019/10/19)
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- TBAI-catalyzed selective synthesis of sulfonamides and β-aryl sulfonyl enamines: coupling of arenesulfonyl chlorides and sodium sulfinates with tert-amines
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A simple, practical and metal-free method has been developed for the synthesis of sulfonamides and β-arylsulfonyl enamines via the selective cleavage of C-N and C-H bonds through the iodine-catalyzed oxidation of arenesulfonyl chlorides and sodium sulfinates with tert-amines. The method uses commercially available inexpensive catalysts and oxidants, and has a wide substrate scope and operational simplicity.
- Jiang, Hongmei,Tang, Xiaoyue,Xu, Zhihui,Wang, Huixian,Han, Kang,Yang, Xiaolan,Zhou, Yuanyuan,Feng, Yong-Lai,Yu, Xian-Yong,Gui, Qingwen
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p. 2715 - 2720
(2019/03/12)
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- High-Throughput Screening and Hit Validation of Extracellular-Related Kinase 5 (ERK5) Inhibitors
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The extracellular-related kinase 5 (ERK5) is a promising target for cancer therapy. A high-throughput screen was developed for ERK5, based on the IMAP FP progressive binding system, and used to identify hits from a library of 57-617 compounds. Four distinct chemical series were evident within the screening hits. Resynthesis and reassay of the hits demonstrated that one series did not return active compounds, whereas three series returned active hits. Structure-activity studies demonstrated that the 4-benzoylpyrrole-2-carboxamide pharmacophore had excellent potential for further development. The minimum kinase binding pharmacophore was identified, and key examples demonstrated good selectivity for ERK5 over p38α kinase.
- Myers, Stephanie M.,Bawn, Ruth H.,Bisset, Louise C.,Blackburn, Timothy J.,Cottyn, Betty,Molyneux, Lauren,Wong, Ai-Ching,Cano, Celine,Clegg, William,Harrington, Ross. W.,Leung, Hing,Rigoreau, Laurent,Vidot, Sandrine,Golding, Bernard T.,Griffin, Roger J.,Hammonds, Tim,Newell, David R.,Hardcastle, Ian R.
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supporting information
p. 444 - 455
(2016/08/16)
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- 1,2-Benzisothiazol-3-one derivatives as a novel class of small-molecule caspase-3 inhibitors
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A novel series of 1,2-benzisothiazol-3-one derivatives was synthesized and their biological activities were evaluated for inhibiting caspase-3 and -7 activities, in which some of them showed low nanomolar potency against caspase-3 in vitro and significant protection against apoptosis in a camptothecin-induced Jurkat T cells system. Among the tested compounds, compound 5i exhibited the most potent caspase-3 inhibitory activity (IC50 = 1.15 nM). The molecular docking predicted the interactions and binding modes of the synthesized inhibitor in the caspase-3 active site.
- Wu, Lixin,Lu, Meiqi,Yan, Zhihui,Tang, Xiaobin,Sun, Bo,Liu, Wei,Zhou, Honggang,Yang, Cheng
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p. 2416 - 2426
(2014/05/06)
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- Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu 4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)
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Herein we disclose the synthesis and SAR of a series of 4-(phenylsulfamoyl)phenylacetamide compounds as mGlu4 positive allosteric modulators (PAMs) that were identified via a functional HTS. An iterative parallel approach to these compounds culminated in the discovery of VU0364439 (11) which represents the most potent (19.8 nM) mGlu4 PAM reported to date.
- Engers, Darren W.,Gentry, Patrick R.,Williams, Richard,Bolinger, Julie D.,Weaver, C. David,Menon, Usha N.,Conn, P. Jeffrey,Lindsley, Craig W.,Niswender, Colleen M.,Hopkins, Corey R.
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scheme or table
p. 5175 - 5178
(2010/10/02)
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- Potent non-nucleoside inhibitors of the measles virus RNA-dependent RNA polymerase complex
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Measles virus (MV) is one of the most infectious pathogens known. In spite of the existence of a vaccine, approximately 350000 deaths/year result from MV or associated complications. Antimeasles compounds could conceivably diminish these statistics and pr
- Sun, Aiming,Yoon, Jeong-Joong,Yin, Yan,Prussia, Andrew,Yang, Yutao,Min, Jaeki,Plemper, Richard K.,Snyder, James P.
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scheme or table
p. 3731 - 3741
(2009/04/10)
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- A new method for the preparation of nitrogen-containing cyclic compounds from p-nitrobenzenesulfonamide and alkyl bis(diphenylphosphinite)s by oxidation-reduction condensation using 1-azidoadamantane
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A new and efficient method was established for the preparation of nitrogen-containing cyclic compounds from p-nitro-benzenesulfonamide, bisphosphinites, and 1-azidoadamantane in good yields under neutral conditions. Copyright
- Mukaiyama, Teruaki,Kuroda, Kiichi,Aoki, Hidenori
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p. 1644 - 1645
(2007/10/03)
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- Neuropeptide Y antagonists
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The compound is a neuropeptide Y antagonist and is effective in treating feeding disorders, cardiovascular diseases and other physiological disorders.
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Page column 37
(2010/02/05)
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