- Facile aromatic nucleophilic substitution (SNAr) reactions in ionic liquids: An electrophile-nucleophile dual activation by [Omim]Br for the reaction
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A facile aromatic nucleophilic substitution (SNAr) reaction in recyclable [Omim]Br under relatively mild conditions has been described. An electrophile-nucleophile dual activation by [Omim]Br is also discovered based on control experiments, 1H NMR and IR spectroscopies. This chemistry provides an efficient and metal-free approach for the generation of Caryl-X (XS, N, O) bonds, many of which are significant synthetic intermediates or drugs, making this methodology attractive to both synthetic and medicinal chemistry.
- Zhang, Xiao,Lu, Guo-Ping,Cai, Chun
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p. 5580 - 5585
(2016/10/21)
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- Synthesis of diaryl ethers, diaryl sulfides, heteroaryl ethers and heteroaryl sulfides under microwave dielectric heating
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This paper describes the synthesis of diaryl ethers and sulfides by utilizing microwave heating methodology. The methodology is shown to be rapid and efficient for the coupling of phenols or thiophenol with electron-deficient aryl halides through a SNAr reaction. The scope of the protocol can be expanded to six-membered heterocycles bearing a hydroxyl group as well as to the reaction of 2-pyrimidinethiol with mildly activated aryl halides, providing heteroaryl ethers and sulfides, respectively. The advantages of the present method include the wide substrate scope, the obviation of metal catalysts, ease of product isolation, and high purity of products. Georg Thieme Verlag Stuttgart.
- Li, Feng,Meng, Qingqing,Chen, Huansheng,Li, Zhiming,Wang, Quanrui,Tao, Fenggang
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p. 1305 - 1313
(2007/10/03)
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- Discovery of FR115092 : A novel antinephritic agent
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A series of dapsone-related 4-aminophenyl and 2-aminothiazolyl derivatives was prepared, and their antinephritic activity and blood toxicity were evaluated. 5-(2-Pyridylsulfonyl)-2-thiazolamine (FR115092,26) was effective against two nephritis models, namely graft-versus-host disease (GVHD) and autoimmune W/BF1 mice, and showed none of the blood toxicity observed with dapsone.
- Ogino, Takashi,Tsuji, Kiyoshi,Tojo, Takashi,Igari, Norihiro,Seki, Nobuo,Sudo, Yu,Manda, Toshitaka,Nishigaki, Fusako,Matsuo, Masaaki
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- Phenylthioheterocyclic derivatives
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Compounds of the formula STR1 wherein n is a integer of 0 to 2; R1 ' and R2 ' are, independently, hydrogen, halogen, trifluoromethyl, lower alkoxy or lower alkyl; and X is pyrimidinyl, thiazolyl or STR2 wherein R is hydrogen, lower alkyl, aryl or ar-lower alkyl; provided that at least one or R1 ' and R2 ' is other than hydrogen, and their pharmaceutically acceptable acid addition salts, and an anti-inflammatory method utilizing a compound of the formula STR3 wherein n is an integer of 0 to 2; R1 and R2 are, independently, hydrogen, halogen, trifluoromethyl, nitro, amino, lower alkylamino, di-lower-alkylamino, lower alkoxy or lower alkyl; and X is pyrimidinyl, thiazolyl or STR4 wherein R is hydrogen, lower alkyl, aryl or ar-lower alkyl; and their pharmaceutically acceptable acid addition salts, are described.
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