- Copper-catalyzed carbochlorination or carbobromination via radical cyclization of aryl amines
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A copper-catalyzed radical carbochlorination or carbobromination is reported. Intramolecular cyclization occurred through aryl radicals generated in situ from bench-stable aryl amines with aqueous hydrogen halides as the halogen sources. A variety of (3-h
- Ouyang, Jianing,Su, Xiaolong,Chen, Yu,Yuan, Yaofeng,Li, Yi
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supporting information
p. 1438 - 1441
(2016/03/12)
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- Cyclizing radical carboiodination, carbotelluration, and carboaminoxylation of aryl amines
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Radical carboiodination of various aryl amines is reported. Aryl diazonium salts, generated in situ from the corresponding aryl amines, are reacted with Bu4NI to provide the corresponding aryl radicals which undergo 5-exo or 6-exo cyclization. Iodine abstraction eventually affords the carboiodinated products in good to excellent yields. If TEMPO is added, the cascade provides the cyclized carboaminoxylation products. Running the reaction in the presence of PhTeTePh affords the phenyltellurated cyclized products.
- Hartmann, Marcel,Studer, Armido
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supporting information
p. 8180 - 8183
(2014/08/18)
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- Transition metal-free activation of allylic acetates toward regioselective S-allylation of thiols
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Allylic acetates have been used as allylating agents under transition metal-free condition toward an economical and sustainable regioselective S-allylation of aromatic and aliphatic thiols in the presence of potassium carbonate in DMF.
- Saha, Amit,Ranu, Brindaban C.
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experimental part
p. 1902 - 1905
(2010/09/07)
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- Synthesis of unsaturated 1,4-heteroatom-containing benzo-fused heterocycles using a sequential isomerization-ring-closing metathesis strategy
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A small library of 1,4-benzodioxins and 4H-1,4-benzoxazines was synthesized from the corresponding bis-allyloxy precursors by way of an initial isomerization to the bis-vinyloxy compounds, followed by a ring-closing metathesis using the second generation Grubbs' catalyst (G2). A related strategy, starting from benzene-1,2-dithiol and 2-mercaptophenol, afforded benzodithiin and 1,4-benzoxathiin, respectively.
- Morgans, Garreth L.,Ngidi, E. Lindani,Madeley, Lee G.,Khanye, Setshaba D.,Michael, Joseph P.,de Koning, Charles B.,van Otterlo, Willem A.L.
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experimental part
p. 10650 - 10659
(2010/01/16)
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- Design and synthesis of cinanserin analogs as severe acute respiratory syndrome coronavirus 3CL protease inhibitors
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The severe acute respiratory syndrome (SARS) coronavirus 3CL protease is an attractive target for the development of anti-SARS drugs. In this paper, cinanserin (1) analogs were synthesized and tested for the inhibitory activities against SARS-coronavirus (CoV) 3CL protease by fluorescence resonance energy transfer (FRET) assay. Four analogs show significant activities, especially compound 26 with an IC50 of 1.06 μM.
- Yang, Qingang,Chen, Lili,He, Xuchang,Gao, Zhenting,Shen, Xu,Bai, Donglu
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scheme or table
p. 1400 - 1405
(2009/09/29)
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- Isomerization and ring-closing metathesis for the synthesis of 6-, 7- and 8-membered benzo- and pyrido-fused N,N-, N,O- and N,S-heterocycles
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An isomerization-ring-closing metathesis (RCM) strategy afforded N-substituted 4H-1,4-benzoxazines from the protected N-allyl-2-(allyloxy) anilines. In addition, RCM was used to synthesize the N-substituted, 8-membered benzo-fused heterocycles from the re
- Van Otterlo, Willem A.L.,Morgans, Garreth L.,Khanye, Setshaba D.,Aderibigbe, Blessing A.A.,Michael, Joseph P.,Billing, David G.
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p. 9171 - 9175
(2007/10/03)
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- A new approach to reductive deprotection of thioethers with a low-valent titanium reagent
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Low-valent titanium mediated cleavage of carbon-sulphur bond is reported. This has resulted in an efficient and mild protocol for the deprotection of allyl/benzyl thioethers under reductive condition and with good yields. Deprotection can be performed regio- and chemo-selectively in the presence of acid, ester and N-benzyl/allyl functionalities and is general for aliphatic and aromatic precursors.
- Shadakshari,Talukdar,Chattopadhyay
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p. 1007 - 1010
(2007/10/03)
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- Synthesis of 4-(Phenylamino)quinoline-3-carboxamides as a novel class of gastric H+/K+-ATPase inhibitors
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In a search for inhibitors of gastric H+/K+-ATPase, 4-(phenylamino)quinoline-3-carboxamides were synthesized and evaluated for antisecretory activity against histamine-induced gastric acid secretion in rats. These compounds were synt
- Uchida,Otsubo,Matsubara,Ohtani,Morita,Yamasaki
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p. 693 - 698
(2007/10/03)
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