- A catalyst-free and additive-free method for the synthesis of benzothiazolethiones from: O -iodoanilines, DMSO and potassium sulfide
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Under catalyst-free and additive-free conditions, a novel, convenient, eco-friendly method for the synthesis of benzothiazolethiones has been developed. The three-component reaction of o-iodoanilines and K2S with DMSO proceeded smoothly and the corresponding benzothiazolethiones were obtained with good isolated yields. Meanwhile, this method could be used for the synthesis of thioureas from primary diamines. Furthermore, mechanism research showed that DMSO not only functioned as a carbon source, but also as a mild oxidant in this reaction.
- Zhu, Xiaoming,Li, Wenguang,Luo, Xiai,Deng, Guobo,Liang, Yun,Liu, Jianbing
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supporting information
p. 1970 - 1974
(2018/05/23)
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- AlCl3-Promoted Synthesis of 2-Mercapto Benzoheterocycles by Using Sodium Dimethyldithiocarbamate as Thiocarbonyl Surrogate
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A simple, expeditious and high-efficiency synthetic method for the AlCl3-mediated one-pot preparation of 2-mercapto benzoheterocycles (2-mercapto benzothiazoles, benzoxazoles and benzimidazoles) is described. By the treatment of a series of S, O and N heteroatoms containing bifunctional molecules with sodium dimethyldithiocarbamate in AlCl3, the desired benzoheterocycles are obtained smoothly. The protocol can also be applied on the synthesis of a series of thiazolidine-2-thiones, imidazolidine-2-thiones. This novel synthetic approach has advantages such as ligand-free, high efficiency, short reaction time, readily available starting materials and simple experimental procedures.
- Liu, Xing,Zhang, Shi-Bo,Dong, Zhi-Bing
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p. 5406 - 5411
(2018/10/20)
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- PROTEIN KINASE REGULATORS
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The present invention provides, in part, novel compounds and pharmaceutically acceptable salts capable of modulating the activity of kinases, including Akt, ERK and MEK. Such modulation affects biological functions, for example, by inhibiting cell proliferation and/or inducing apoptosis. Also provided are pharmaceutical compositions and medicaments, comprising the compounds or salts of the invention, alone or in combination with other therapeutic agents or palliative agents.
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Page/Page column 59
(2018/03/06)
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- Thiocarbonyl Surrogate via Combination of Sulfur and Chloroform for Thiocarbamide and Oxazolidinethione Construction
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An efficient and practical thiocarbonyl surrogate via combination of sulfur and chloroform has been developed. A variety of thiocarbamides and oxazolidinethiones have been established, including chiral thiourea catalysts and chiral oxazolidinethione auxiliaries with high selectivity. Meanwhile, pesticides Diafenthiuron (an acaricide), ANTU (a rodenticide), and Chloromethiuron (an insecticide) were practically synthesized through this method in gram scale. Dicholorocarbene, as the key intermediate, was further confirmed via a carbene-trapping control experiment.
- Tan, Wei,Wei, Jianpeng,Jiang, Xuefeng
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supporting information
p. 2166 - 2169
(2017/04/27)
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- An environmentally benign and efficient synthesis of substituted benzothiazole-2-thiols, benzoxazole-2-thiols, and benzimidazoline-2-thiones in water
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An efficient and practical method for the one-step synthesis of benzothiazole-2-thiols, benzoxazole-2-thiols and benzimidazoline-2-thiones by cyclization of 2-aminothiophenols, 2-aminophenols, and 1,2-phenylenediamines with tetramethylthiuram disulfide (TMTD) in water was described. The features of this method include metal/ligand-free, excellent yield, short reaction time and broad substrate scope. The method provides a facile and convenient preparation of some potentially biologically active compounds.
- Liu, Xing,Liu, Min,Xu, Wan,Zeng, Meng-Tian,Zhu, Hui,Chang, Cai-Zhu,Dong, Zhi-Bing
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p. 5591 - 5598
(2017/12/06)
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- A simple route for the synthesis of symmetrical thiourea derivatives and amidinium cations by reaction between isocyanides, amines and carbon disulfide
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Reaction between primary amines and CS2 promoted by alkyl isocyanides in ethanol as solvent provides a simple and efficient route for the synthesis of symmetrical thiourea derivatives. The reaction of secondary amines with carbon disulfide and alkyl isocyanides afforded new amidinium cations in good yields.
- Anary-Abbasinejad, Mohammad,Karimi, Nadia,Mehrabi, Hossein,Ranjbar-Karimi, Reza
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p. 653 - 659
(2013/02/22)
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- Bifunctional Chiral Auxiliaries 5: The Synthesis of 1,3-Diacylimidazolidine-2-thiones and 1,3-Diacylimidazolidin-2-ones from 1,2-Diamines
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Although 1,2-diamines fail to cyclise with urea, phosgene or 1,1'-carbonyl diimidazole, they react with carbon disulphide to give the corresponding imidazolidine-2-thiones.These undergo clean diacylation to give 1,3-diacylimidazolidine-2-thiones which are
- Davies, Stephen G.,Mortlock, Andrew A.
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p. 4419 - 4438
(2007/10/02)
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- Bifunctional chiral auxiliaries 2: The synthesis of 1,3-diacylimidazolidin-2-ones from 1,2-diamines
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The title compounds are readily prepared in three steps via the corresponding 1,3-diacylimidazolidine-2-thiones. The final step involves the novel use of mercury (II) acetate for the conversion of thioureas to ureas.
- Davies,Mortlock
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p. 4791 - 4794
(2007/10/02)
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- Effect of Structural Change on Acute Toxicity and Antiinflammatory Activity in a Series of Imidazothiazoles and Thiazolobenzimidazoles
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The effect of structural change on the biological activity of a series of imidazothiazoles and thiazolobenzimidazoles is described.It was found that compounds with polar substituents at the 2 or 3 position of the ring system are less acutely toxic while maintaining antiinflammatory activity.Other structural changes, such as the incorporation of a gem-dimethyl substituent in the 6 position, increase acute toxicity and eliminate antiinflammatory activity.The compound with the best activity/toxicity ratio contains an alkyl sulfonyl substituent on the thiazole ring.The thiazolobenzimidazole analogues are more potent than the imidazole analogues.
- Powers, Larry J.,Fogt, S. W.,Ariyan, Z. S.,Rippin, D. J.,Heilman, R. D.,Matthews, Richard J.
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p. 604 - 609
(2007/10/02)
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- Tetracyclic imidazo [2,1-b] quinazolinone derivatives
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Disclosed are compounds which are tetracyclic derivatives of imidazo[2,1-b]quinazolinones, e.g., 6-(p-fluorobenzyl)-1,2,3,4,4a,12a-hexahydrobenzimidazo[2,1-b]quinazolin-11(6H)-one. The compounds are also useful as bronchodilator agents, and certain compounds are also useful as tranquillizers and sedative/hypnotic agents. The compounds may be prepared by reacting an isatoic anhydride with a 2-organomercapto-hexahydrobenzimidazole or hexahydrocyclopentimidazole such as 3a,4,5,6,7,7a-hexahydro-2-mercaptomethyl-3H-benzimidazole.
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