- Xanthates as Thiol Surrogates for Nucleophilic Substitution with Aryl Halides
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We herein report an unprecedented xanthate-based protocol for the preparation of aryl-alkyl thioethers. Heating xanthates with aryl halides and namely cesium carbonate in methanol provides the target thioethers in generally good yields within short reaction times. This method allows one to avoid contact with odorous thiols and also to introduce substituents of which the corresponding thiols are virtually unavailable or inconvenient in use.
- Sokolov, Anatolii I.,Mikhaylov, Andrey A.,Baleeva, Nadezhda S.,Baranov, Mikhail S.
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p. 4350 - 4357
(2021/08/24)
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- Polycyclic N-heterocyclic compounds. Part 84: Reaction of N-(pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-yl)amidines or N-(pyrido[2',3':4,5]furo[3,2-d]pyrimidin-4-yl)amidines with hydroxylamine hydrochloride
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The reactions of nine N-(pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-yl)amidines (3) with hydroxylamine hydrochloride produced new cyclization products. These were formed via ring cleavage of the pyrimidine component followed by a 1,2,4-oxadiazole-forming r
- Okuda, Kensuke,Ide, Ryota,Uramaru, Naoto,Hirota, Takashi
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p. 880 - 887
(2015/05/13)
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- Synthesis and biological evaluation of N-arylbenzo[b]thieno[3,2-d] pyrimidin-4-amines and their pyrido and pyrazino analogues as Ser/Thr kinase inhibitors
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A useful and rapid access to libraries of N-arylbenzo[b]thieno[3,2-d] pyrimidin-4-amines and their pyrido and pyrazino analogues was designed and optimized for the first time via microwave-accelerated condensation and Dimroth rearrangement of the starting anilines with N′-(2-cyanoaryl)-N,N- dimethylformimidamides obtained by reaction of thiophene precursors with dimethylformamide dimethylacetal. The inhibitory potency of the final products against five protein kinases (CDK5/p25, CK1δ/ε, GSK3α/β, DYRK1A and CLK1) was estimated. N-arylpyrido[3′,2′:4,5]thieno[3,2-d] pyrimidin-4-amine series of compounds (4a-j) turned out to be particularly promising for the development of new pharmacological inhibitors of CK1 and CLK1 kinases.
- Loidreau, Yvonnick,Marchand, Pascal,Dubouilh-Benard, Carole,Nourrisson, Marie-Renée,Duflos, Muriel,Lozach, Olivier,Loa?c, Nadège,Meijer, Laurent,Besson, Thierry
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p. 171 - 183
(2013/02/22)
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- Synthesis and antifungal activity of pyrido[3',2':4,5]thieno[3,2-d]-1,2,3-triazine derivatives
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The antimicrobical activity of some pyrido[3'2':4,5]thieno[3,2d]-1,2,3-triazine derivatives has been studied. Some compounds proved effective against microorganisms in vitro, compounds 3a and 3c in particular exhibited antifungal activity, comparable to M
- Guerrera,Salerno,Sarva,Siracusa,Oliveri,Minardi
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p. 1725 - 1733
(2007/10/02)
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