- Iodine/DMSO-Promoted Selective Direct Arylthiation of Anilines with Thiols under Metal-Free Conditions
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An iodine-promoted divergent thiolation of unprotected anilines with thiols for the synthesis of sulfide anilines has been described. The combinational use of I2 and DMSO played an important role to realize this kind of transformation without the aid of a
- Zhao, Wenqi,Zhang, Feng,Deng, Guo-Jun
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p. 291 - 301
(2021/01/14)
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- Flavin/I2 catalyzed aerobic oxidative C–H sulfenylation of anilines
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A flavin/I2 catalyzed aerobic oxidative C–H sulfenylation of anilines with thiols under mild reaction conditions is presented for the first time. This metal-free reaction provides an atom-economic pathway to prepare various aryl sulfides with outstanding functional group compatibility. Moreover, it consumes molecular oxygen as the only terminal oxidant and produces environmentally-friendly H2O as the only byproduct.
- Jiang, Xinpeng,Shen, Zhifeng,Zheng, Cong,Fang, Liyun,Chen, Keda,Yu, Chuanming
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supporting information
(2020/07/24)
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- CoII immobilized on an aminated magnetic metal-organic framework catalyzed C-N and C-S bond forming reactions: A journey for the mild and efficient synthesis of arylamines and arylsulfides
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In this work, we report a simple and versatile method for the modification of a metal-organic framework (NH2-MIL53(Al)) in a step-wise manner. To characterize the synthesized nanostructured catalyst, a variety of spectroscopic and microscopic techniques including FT-IR, XRD, BET, TEM, FE-SEM, EDX, EDX-mapping, TGA, XPS, VSM, ICP-OES and CHN have been employed. Fe3O4@AMCA-MIL53(Al)-NH2-CoII NPs, which benefit from small nanocrystalline size (10-30 nm, according to the XRD and TEM data) in combination with the coexistence of magnetic nanoparticles, a metal-organic framework, and cobalt species, were found to be an excellent environment catalyst to promote the C-N and C-S cross coupling reactions. A wide range of functional substrates including electron-withdrawing and electron-donating aryl halides underwent the coupling reaction with aromatic/heteroaromatic/benzylic and aliphatic amines and sulfides. The results demonstrated that the yields of the target products were good to excellent and the catalyst can be recycled for at least seven recycling runs without a discernible decrease in its catalytic activity. Furthermore, the heterogeneity studies (such as hot filtration and poisoning tests) efficiently confirmed that the as-synthesized nanostructured catalyst is heterogeneous and completely stable under the reaction conditions. We hope that our study inspires more interest in designing novel catalysts based on using low-cost metal ions (such as cobalt) in the field of cross coupling reactions.
- Mohammadinezhad, Arezou,Akhlaghinia, Batool
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p. 15525 - 15538
(2019/10/19)
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- Metal-Free Iodine-Catalyzed Direct Arylthiation of Substituted Anilines with Thiols
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Iodine-catalyzed direct arylthiation of substituted anilines for the synthesis of various diaryl sulfides has been developed under metal- and solvent-free conditions. The present method uses readily available thiols as the arylthiation reagents, and envir
- Yang, Daoshan,Yan, Kelu,Wei, Wei,Zhao, Jing,Zhang, Mengqi,Sheng, Xuguang,Li, Guoqing,Lu, Shenglei,Wang, Hua
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p. 6083 - 6092
(2015/06/30)
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- Arylthiolation of arylamine derivatives with (arylthio)-pyrrolidine-2,5-diones
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A simple and efficient method for arylthiolation of arylamines has been developed. The protocol uses (arylthio)pyrrolidine-2,5-diones as the arylthiolating reagents, acetonitrile as the solvent, and no catalyst and additive are required, which avoids contamination from the transition metal catalysts in the target products. Therefore, the present method should provide a convenient, efficient and practical strategy for the synthesis of other aryl sulfides.
- Tian, Hua,Yang, Haijun,Zhu, Changjin,Fu, Hua
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supporting information
p. 481 - 488
(2015/03/05)
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- 4- { [ ( PYRIDIN- 3 - YL -METHYL) AMINOCARBONYL] AMINO} BENZENE - SULFONE DERIVATIVES AS NAMPT INHIBITORS FOR THERAPY OF DISEASES SUCH AS CANCER
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The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An embodiment of the invention is the provision of a compound of Formula IIIA.
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Page/Page column 234
(2012/03/26)
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- FeF3/i2-catalyzed synthesis of 4-chalcogen- substituted arylamines by direct thiolation of an arene C-H bond
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An efficient regioselective synthesis of 4-chalcogen-substituted-arylamines by FeF3-catalyzed sulfenylation and selenation of arylamines has been developed. In the presence of FeF3and I2, a variety of arylamines underwent the reaction with disulfides or diselenides to afford the corresponding 4-sulfenyl-or 4-selenenyl-arylamines in moderate to good yields. Georg Thieme Verlag Stuttgart.
- Fang, Xiao-Li,Tang, Ri-Yuan,Zhang, Xing-Guo,Li, Jin-Heng
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experimental part
p. 1099 - 1105
(2011/05/14)
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- GLYT2 MODULATORS
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α-, β-, and γ-amino acid derivatives of formula I are disclosed as selective GlyT2 inhibitors for the treatment of central nervous system (CNS) conditions such as muscle spasticity, tinnitus, epilepsy and neuropathic pain. Formula I
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Page/Page column 113
(2010/02/11)
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- Discovery and SAR development of 2-(phenylamino) imidazolines as postacyclin receptor antagonists
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On the basis of screening hits (1a,b), a series of selective, high affinity prostacyclin receptor antagonists was developed. The optimized lead compound 25d [(4,5-dihydro-1H-imidazol-2-yl)-[4-(4-isopropoxybenzyl)phenyl] amine] had analgesic activity in the rat.
- Clark, Robin D.,Jahangir, Alam,Severance, Daniel,Salazar, Rick,Chang, Thomas,Chang, David,Jett, Mary Frances,Smith, Steven,Bley, Keith
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p. 1053 - 1056
(2007/10/03)
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- Magenta-masked color azopyrazolinone couplers
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Orange colored magenta color couplers of the general formula STR1 are provided, in which R is optionally substituted alkyl, aralkyl, aryl or a heterocyclic group, X is optionally substituted aryl, Y is optionally substituted acyl-amino, aroyl amino or aryl amino and Z represents further optional substituents of the phenyl ring. Preferably Y also contains a ballasting group, which is a long claim alkyl group having 10 to 24 carbon atoms in the chain.
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