- In vitro anti-Candida activity and action mode of benzoxazole derivatives
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A newly synthetized series of N-phenacyl derivatives of 2-mercaptobenzoxazole, including analogues of 5-bromo- and 5,7-dibromobenzoxazole, were screened against Candida strains and the action mechanism was evaluated. 2-(1,3-benzoxazol-2-ylsulfanyl)-1-(4-b
- ?ukowska-Chojnacka, Edyta,Baran, Joanna,Gryciuk, Aleksander,Kawalec, Joanna,Kowalkowska, Anna,Kuryk, ?ukasz,Rogalska, Marta,Staniszewska, Monika
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- Zinc oxide catalyzed solvent-free mechanochemical route for C-S bond construction: A sustainable process
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A zinc oxide catalyzed solvent-free mechanochemical process has been developed for the rapid construction of C-S bonds by using a nucleophilic substitution reaction (SN2 mechanism) that involves a variety of thiols and phenacyl/ benzyl/alkyl bromides. Notable advantages of this method in-clude its broad substrate scope, clean reaction profile, safety, scalability, high product yields at ambient conditions, and the recyclability of the catalyst. Furthermore, the prepared compounds are valuable building blocks for the synthesis of various biologically active molecules.
- Md. Khaja Mohinuddin,Gangi Reddy
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p. 1207 - 1214
(2017/12/07)
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- Preparation method of alpha-heterocycle sulfide ketone compound
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The invention provides a method for efficiently synthesizing different heterocycle sulfide ketone derivatives. According to the method, KI is adopted as a catalyst, potassium persulfate is adopted as an oxidizing agent, a carbonyl compound and benzoheterocycle mercaptan are taken as reaction substrates at room temperature, and DMSO is added into a reaction system as a solvent. The method provided by the invention has the advantages that the catalyst is cheap and available; reaction conditions are mild, and reaction can be carried out at room temperature, thereby being safe and reliable; and the highest yield of the obtained target product reaches 94%. The method provided by the invention overcomes the defects that a substrate of the traditional heterocycle thio etherification reaction is expensive, multi-step reaction is required to be carried out and reaction conditions are harsh, and the method provided by the invention has a good industrial application prospect.
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Paragraph 0034; 0035
(2017/08/30)
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- KI/K 2 S 2 O 8 -Mediated α-C-H Sulfenylation of Carbonyl Compounds with (Hetero)Aryl Thiols
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A new and facile KI/K 2 S 2 O 8 -mediated α-C-H sulfenylation of carbonyl compounds with (hetero)aryl thiols was developed for the formation of C-S bond at room temperature. This method provided a simple process for the sy
- Yang, Zan,Li, Jiao,Hua, Jie,Yang, Tao,Yi, Jianmin,Zhou, Congshan
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supporting information
p. 2325 - 2329
(2017/10/06)
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- Synthesis of α-sulfenyl monoketones: Via a metal-free oxidative cross dehydrogenative coupling (CDC) reaction
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α-Sulfenyl ketones are potential precursors which find a variety of applications in organic synthesis. Their typical synthesis requires pre-functionalized starting materials and two to three step synthetic sequences. In addition, the selective pre-functionalization of unsymmetrical ketones is a challenge, which limits the synthesis of the desired sulfenylated ketones. To overcome these disadvantages, a metal-free, convenient one-step strategy for synthesizing α-sulfenyl ketones at ambient temperature via a cross-dehydrogenative coupling (CDC) strategy has been developed with a broad substrate scope. Therefore, this CDC strategy for C-S bond formation is attractive and may find wide applications in organic synthesis.
- Varun, Begur Vasanthkumar,Gadde, Karthik,Prabhu, Kandikere Ramaiah
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supporting information
p. 7665 - 7670
(2016/08/24)
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- Synthesis of difluorinated β-ketosulfones and novel gem-difluoromethylsulfone-containing heterocycles as fluorinated building blocks
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A series of new heterocyclic β-ketosulfides was prepared by the reaction of the corresponding heterocyclic thiols with α-bromoacetophenone and its derivatives. Oxidation of the products using m-CPBA gave the corresponding heterocyclic β-ketosulfones, whic
- Loghmani-Khouzani, Hossein,Hajiheidari, Dariush
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experimental part
p. 561 - 569
(2010/05/18)
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- BENZOXAZOLINONES. VI. REACTION OF BENZOXAZOLINONE AND OF BENZOAZOLINETHIONE WITH SUBSTITUTED α-HALO CARBONYL COMPOUNDS
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The alkylation of the potassium and triethylammonium salts of benzoxazolinones and benzoxazolinethiones with α-halo carbonyl compounds has been studied.The reaction takes place at the less electronegative atoms of the ambident benzoxazolinone and benzoxazolinethione anions.On the nitration of 3-phenacylbenzoxazoline moiety of the molecule.
- Aflyatunova, R. G.,Babakhanova, Kh. R.,Aliev, N. S.
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p. 340 - 344
(2007/10/02)
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- RING TRANSFORMATIONS OF OXAZOLES AND THEIR BENZO ANALOGUES. NEW SYNTHETIC ROUTE FOR 2H-IMIDAZOTHIADIAZINE AND N-HETEROARYL-o-AMINOPHENOL
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Ring transformations of certain functionalized oxazoles and their benzo analogues were studied.The α-(oxazol-2-ylthio) ketones 3a, b, c, and e gave 2H-imidazothiadiazines (4a, b, c, and e) on treatment with hydrazine hydrate in acetic acid.S
- Sasaki, Tadashi,Ito, Eikoh,Shimizu, Ikuo
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p. 2119 - 2129
(2007/10/02)
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