- Studies on pyrazine derivatives, XLV: Synthesis, reactions, and tuberculostatic activity of N-methyl-N′-(pyrazine-2-carbonyl)- hydrazinecarbodithioic acid methyl ester
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Methyldithiocarbonyl derivative 2 of pyrazine-2-carboxylic acid N′-methylhydrazide 1 was synthesized by methylation of CS2 adduct. Benzylamine caused the decomposition of compound 2 to pyrazine-2-carboxylic acid benzylamide 5 and 1,3-dibenzylthiourea, 6. N-methyl-N'′-(pyrazine-2-carbonyl)-hydrazinecarbodithioic acid methyl ester 2 were evidenced to cyclize to 3-methyl-5-pyrazin-2-yl-3H-[1,3,4] oxadiazole-2-thione 8 in the presence of triethylamine. In the reactions with secondary amines such as morpholine, pyrrolidine and phenylpiperazine pyrazinoyl derivatives (9-11) of thiosemicarbazide were obtained. Hydrazine, methylhydrazine, aminoalcohols, and N-alkylamino-substituted cyclic amines reacted with cyclization to 4-substituted 1,2,4-triazole-3-thiones 12, 13, and 18-22. Synthesized compounds exhibited low tuberculostatic activity in vitro (MIC 50-100 μg/mL). Copyright Taylor & Francis Group, LLC.
- Gobis, Katarzyna,Foks, Henryk,Zwolska, Zofia,Augustynowicz-Kopec, Ewa
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Read Online
- Method for preparing N,N'-dicyclohexylcarbodiimide by using co-reactor
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The invention discloses a method for preparing N,N'-dicyclohexylcarbodiimide by using a co-reactor. The method comprises the steps of maintaining an aqueous solution of cyclohexylamine in a strong alkaline environment in the same reactor, adding carbon disulfide into the same reactor, and adding sodium hypochlorite for oxidation to obtain N,N'-dicyclohexylcarbodiimide. According to the method, thetechnological process is simplified through the co-reactor reaction, generation of highly toxic and harmful gas is avoided, the safety risk of production is reduced, and then the purpose of environment-friendly and safe production is achieved.
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Paragraph 0043-0045
(2021/03/30)
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- Nickle Catalysis Enables Access to Thiazolidines from Thioureas via Oxidative Double Isocyanide Insertion Reactions
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An efficient synthesis of thiazolidine-2,4,5-triimine derivatives was developed via Ni-catalyzed oxidative double isocyanide insertion to thioureas under air conditions, in which thioureas play three roles as a substrate, a ligand, and overcoming isocyanide polymerization. The reaction is featured by employing a low-cost and low loading Ni(acac)2 catalyst, without any additives, and high atom economy. This is the first example to directly apply a Ni(II) catalyst in oxidative double isocyanide insertion reactions.
- Yuan, Wen-Kui,Liu, Yan Fang,Lan, Zhenggang,Wen, Li-Rong,Li, Ming
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supporting information
p. 7158 - 7162
(2018/11/25)
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- Rapid and highly efficient synthesis of thioureas in biocompatible basic choline hydroxide
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A straightforward and convenient synthesis of symmetrical thiourea derivatives by the reaction of primary amines and carbon disulfide in biocompatible basic choline hydroxide is presented. A variety of biologically important thiourea derivatives can be obtained in good to excellent yields without a tedious work-up under mild reaction conditions. A series of primary aliphatic and aromatic amines with different substituted functional groups have been converted to thiourea derivatives under milder reaction conditions and short reaction times.
- Azizi, Najmedin,Farhadi, Elham
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p. 548 - 554
(2017/09/27)
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- Method for recycling recycled N,N'-dicyclohexylurea
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The invention relates to a method for recycling recycled N,N'-dicyclohexylurea. The method comprises the steps of adding N,N'-dicyclohexylurea and sodium hydroxide into a reaction still, starting stirring, raising temperature to 80-450 DEG C and reacting for 2-8 hours to steam out yielded fluid of cyclohexane in a reaction process. The method has the advantages that the N,N'-dicyclohexylurea of a bio-polypeptide condensing agent by-product is recycled to achieve reclamation of wastes, the problem that the industrialization of the N,N'-dicyclohexylurea is hard to be processed is solved, and the regeneration from the N,N'-dicyclohexylurea to cyclohexylamine to N,N'-dicyclohexylcarbodiimide is achieved, a solvent is not used, and the shortcomings that an organic solvent is flammable and combustible and high in cost are overcome, the yield of the cyclohexylamine is larger than 99%, the purity is larger than 99.3%, raw materials only have the N,N'-dicyclohexylurea and the sodium hydroxide, the products are only cyclohexylamine and sodium carbonate, and the cyclohexylamine and the sodium carbonate can be separated easily. The method is safe and environmentally friendly, low in cost and suitable for industrial production.
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Paragraph 0027
(2016/10/31)
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- Green process development for the synthesis of aliphatic symmetrical N,N'-disubstituted thiourea derivatives in aqueous medium
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A highly efficient green process for the synthesis of N,N'-disubstituted aliphatic thiourea derivatives using primary aliphatic amines and carbon disulfide in aqueous medium at room temperature via a nonisothiocyanate route is described. This protocol illustrates the rapid preparation of N,N'-disubstituted aliphatic thiourea derivatives in excellent yields with some advantages such as no catalyst and simple workup without any side product formation. Moreover the new route is concise, chromatography-free, and adaptable to pilot-scale preparation.
- Jangale, Asha D.,Kumavat, Priyanka P.,Wagh, Yogesh B.,Tayade, Yogesh A.,Mahulikar, Pramod P.,Dalal, Dipak S.
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supporting information
p. 236 - 244
(2015/10/29)
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- Green Process Development for the Synthesis of Aliphatic Symmetrical N,N ′-Disubstituted Thiourea Derivatives in Aqueous Medium
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A highly efficient green process for the synthesis of N,N′-disubstituted aliphatic thiourea derivatives using primary aliphatic amines and carbon disulfide in an aqueous medium at room temperature via a nonisothiocyanate route is described. This protocol illustrates the rapid preparation of N,N′-disubstituted aliphatic thiourea derivatives in excellent yields with some advantages such as no catalyst and simple workup without any side product formation. Moreover, the new route is concise, does not require chromatography, and is adaptable to pilot-scale preparation. GRAPHICAL ABSTRACT.
- Jangale, Asha D.,Kumavat, Priyanka P.,Wagh, Yogesh B.,Tayade, Yogesh A.,Mahulikar, Pramod P.,Dalal, Dipak S.
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supporting information
p. 376 - 385
(2015/10/29)
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- Application of "hydrogen bonding interaction" in new drug development: Design, synthesis, antiviral activity, and sars of thiourea derivatives
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A series of simple thiourea derivatives were designed based on the structure of natural product harmine and lead compound and synthesized from amines in one step. The antiviral activity of these thiourea derivatives was evaluated. Most of them exhibited significantly higher anti-TMV activity than commercial plant virucides ribavirin, harmine, and lead compound. The hydrogen bond was found to be important but not the more the better. The optimal compound (R,R)-20 showed the best anti-TMV activity in vitro and in vivo (in vitro activity, 75%/500 a??g/mL and 39%/100 a??g/mL; inactivation activity, 71%/500 a??g/mL and 35%/100 a??g/mL; curative activity, 73%/500 a??g/mL and 37%/100 a??g/mL; protection activity, 69%/500 a??g/mL and 33%/100 a??g/mL), which is significantly higher than that of Ningnanmycin. The systematic study provides strong evidence that these simple thiourea derivatives could become potential TMV inhibitors.
- Lu, Aidang,Wang, Ziwen,Zhou, Zhenghong,Chen, Jianxin,Wang, Qingmin
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p. 1378 - 1384
(2015/03/05)
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- Synthesis of thioureas in ionic liquid medium
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A highly efficient procedure for the synthesis of symmetrical thioureas by means of simple condensation of primary amines and carbon disulfide in 1-butyl-3-methylimidazolium chloride [BMIM][Cl] as a cheap and commercially available ionic liquid is presented. This procedure works for aromatic and aliphatic primary amines and give high to excellent yields of symmetrical thioureas without need for any catalyst or tedious work-up.
- Halimehjani, Azim Ziyaei,Farahbakhsh, Fataneh
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p. 284 - 288
(2013/08/26)
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- Copper-catalyzed one-pot synthesis of 2-thioxo-2,3-dihydroquinazolin-4(1H)- ones from ortho-bromobenzamides and isothiocyanates
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Copper-catalyzed tandem reaction of ortho-bromobenzamides and isothiocyanates is described, which provides an efficient and practical route for the synthesis of 2-thioxo-2,3-dihydroquinazolin-4(1H)-ones. The optimal condition involved the following parameters: CuI as precatalyst, Cs 2CO3 as base, N,N′-dimethylethane-1,2-diamine as ligand, and toluene as solvent, with reaction temperature at 120 °C.
- Wang, Fei,Zhao, Peng,Xi, Chanjuan
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supporting information; experimental part
p. 231 - 235
(2011/02/28)
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- Exploration of novel 2-alkylimino-1,3-thiazolines: T-type calcium channel inhibitory activity
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We have developed combinatorial libraries of new 2-alkylimino-1,3- thiazolines with four diversity points, consisting of more than 500 compounds, in a parallel synthetic fashion. The synthetic strategy was based on the construction of a large library aimed at the discovery of new compounds with T-type calcium channel inhibitory activity through structure modifications of hit compound 2. The syntheses of the compounds of Chemset A with four diversity points were accomplished by the condensation of thioureas 5 with α-haloketones 6{1-66} having two diversity points each. A library of phthalimidyl 1,3-thiazolines 24 was synthesized to provide Chemset B, which allowed the introduction of other diversity points through the nucleophilic character of the amino nitrogen. A sublibrary, Chemset C, was constructed from the libraries of Chemset A and Chemset B by functionalization of the C-4 position of the 1,3-thiazoline ring. The products containing ester or acid groups at the C-4 position of the 1,3-thiazoline ring were used in amide synthesis to give a new sublibrary within Chemset C. Deprotection of the phthalimidyl moiety of 24 followed by the reaction with benzoyl chloride gave the corresponding sublibrary in Chemset C. Another sublibrary which includes secondary amino derivatives was obtained by reduction of the amide moiety or reductive amination of 23 with phenyl aldehyde. The selected compounds from the generated libraries were evaluated with respect to inhibition of T-type calcium channels, where some of them have exhibited promising activity.
- Han, Minsoo,Nam, Kee Dal,Shin, Dongyun,Jeong, Nakcheol,Hahn, Hoh-Gyu
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experimental part
p. 518 - 530
(2010/08/20)
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- Novel thiofomylation of primary and secondary amines using N-aryl-1,2,3,4,5,7-pentathiazocanes
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Heating of N-aryl-1,2,3,4,5,7-pentathiazocanes 1 in the presence of primary and secondary amines afforded N-Alkyl or N,N-dialkylthioformamides 5, and similar heating of 1 in the absence of amines afforded an inseparable mixture of acyclic polysulfides 4 bearing a thioformanilide moiety on each terminal. Bisthioformanilides 4 were also converted into 5 by treating with these amines, and the thioformylation was assumed to proceed through a pathway involving the ring fission of 1 and the subsequent nucleophilic attack of these amines onto the thioformyl group of 4. Copyright Taylor & Francis Group.
- Shimada, Kazuaki,Shibuya, Hiroki,Makino, Kenshiro,Otsuka, Tatsuya,Onuma, Yuki,Aoyagi, Shigenobu,Takikawa, Yuji
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scheme or table
p. 1077 - 1089
(2010/09/04)
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- Efficient method of synthesis of N,N′-disubstituted ureas/thioureas by a Zinc chloride catalyzed thermal reaction
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Symmetrically N,N'-disubstituted ureas/thioureas were synthesized by heating amines or phenyl hydrazine and urea/thiourea on a preheated hot plate at 80-85C under solvent-free conditions in the presence of a catalytic amount of ZnCl2 as a catalyst. The protocol has the advantages of not using toxic phosgene and other hazardous substrates or organic solvents. Increased reaction rate, good yield, and a simple workup procedure are involved.
- Pasha,Madhusudana Reddy
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experimental part
p. 2928 - 2934
(2009/12/03)
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- Efficient synthesis of N,N′-disubstituted ureas/thioureas catalyzed by iodine
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Iodine is an efficient catalyst for the synthesis of symmetrically N,N′-disubstituted ureas/thioureas by heating respective amines or phenyl hydrazine and urea/thiourea on a preheated hot plate at 90-95°C, under solvent-free conditions. The yields are excellent, and the reactions go to complete within 5-10 min. Copyright Taylor & Francis Group, LLC.
- Pasha,Jayashankara
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p. 1787 - 1793
(2007/10/03)
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- MCM-41-TBD as a new, efficient, supported heterogeneous catalyst for the synthesis of thioureas
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The preparation of thioureas, by reaction of carbon disulfide with primary amines, can be efficiently catalyzed, under heterogeneous conditions, by MCM-TBD as a new and reusable catalyst.
- Ballini, Roberto,Bosica, Giovanna,Fiorini, Dennis,Maggi, Raimondo,Righi, Paolo,Sartori, Giovanni,Sartorio, Raffaella
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p. 8445 - 8447
(2007/10/03)
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- Cyanoguanidines as cell proliferation inhibitors
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The present invention relates to hitherto unknown compounds of formula (I) or their tautomeric forms, the attachment to the pyridine ring being in the 3- or 4-position, in which formula R1 stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, halogen, trifluoromethyl, carboxy, C1-C4 alkyl, alkoxy or alkoxycarbonyl, nitro, amino or cyano and Q stands for C4-C20 divalent hydrocarbon radical which can be straight, branched, cyclic, saturated or unsaturated and X stands for carbonyl, carbonylamino, aminocarbonyl, oxycarbonyloxy, oxycarbonyl, carbonyloxy, aminocarbonyloxy, aminothiocarbonyloxy, oxycarbonylamino or oxythiocarbonylamino and Y stands for benzylene or phenylene and R2 stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, C1-C4 alkyl, hydroxyalkyl or alkoxy, hydroxy, halogen, trifluoromethyl, cyano, carboxamido, sulfamoyl, nitro, amino, carboxy, alkoxycarbonyl or benzyloxy; and pharmaceutically acceptable, non-toxic salts and N-oxides thereof. The present compounds are of value in the human and veterinary practice.
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Page column 5-6
(2008/06/13)
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- Development of a pharmacophore model for histamine H3 receptor antagonists, using the newly developed molecular modeling program SLATE
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New molecular modeling tools were developed to construct a qualitative pharmacophore model for histamine H3 receptor antagonists. The program SLATE superposes ligands assuming optimum hydrogen bond geometry. One or two ligands are allowed to flex in the procedure, thereby enabling the determination of the bioactive conformation of flexible H3 antagonists. In the derived model, four hydrogen-bonding site points and two hydrophobic pockets available for binding antagonists are revealed. The model results in a better understanding of the structure-activity relationships of H3 antagonists. To validate the model, a series of new antagonists was synthesized. The compounds were designed to interact with all four hydrogen-bonding site points and the two hydrophobic pockets simultaneously. These ligands have high H3 receptor affinity, thereby illustrating how the model can be used in the design of new classes of H3 antagonists.
- De Esch,Mills,Perkins,Romeo,Hoffmann,Wieland,Leurs,Menge,Nederkoorn,Dean,Timmerman
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p. 1666 - 1674
(2007/10/03)
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- Thiocarbamoylation of amine-containing compounds 5. The mechanism of reactions of tetramethylthiuram disulfide with aliphatic amines
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Thiocarbamoylation of aliphatic amines with tetramethylthiuram disulfide (TMTD) was studied. The reactions were established to proceed according to a two-stage mechanism. In the first stage, S-(thiocarbamoyl)thiohydroxylamines and dimethyl dithiocarbamates are formed. The latter exist in equilibrium with dimethyldithiocarbamic acid, which can undergo decomposition to give dimethylamine and carbon disulfide. In the second stage, several competitive transformations of these intermediates into the final products occur, viz., (1) the reactions of CS2 with primary amines on heating (70-110 deg C) yield mixed and symmetrical thioureas and the reactions of CS2 with secondary amines give symmetrical dithiocarbamates, and (2) insertion of CS2 into S-(thiocarbamoyl)thiohydroxylamines affords thiuram disulfides. Thiuram disulfides formed from primary amines decompose to give isothiocyanates, which are converted into thioureas by condensation with amines, whereas thiuram disulfides which are obtained in the reactions with secondary amines and which cannot form thioureas react with amines analogously to TMTD.
- Boi, Luu Van
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p. 335 - 343
(2007/10/03)
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- 1-(Methyldithiocarbonyl)imidazole: A useful thiocarbonyl transfer reagent for synthesis of substituted thioureas
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1-(Methyldithiocarbonyl)imidazole 1 and its N-methyl quaternary salt 2 have been shown to be efficient methyldithiocarbonyl and thiocarbonyl transfer reagents for the synthesis of dithiocarbamates, symmetrical and unsymmetrical mono-, di- and tri-substituted thioureas in high yields under mild and simple non-hazardous reaction conditions. (C) 2000 Elsevier Science Ltd.
- Mohanta, Pramod K.,Dhar, Sanchita,Samal,Ila,Junjappa
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p. 629 - 637
(2007/10/03)
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- A convenient method for the preparation of primary and symmetrical N,N'-disubstituted thioureas
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A convenient process for the preparation of both primary thioureas 2 and symmetrical N,N'-disubstituted thioureas 6 based on the condensation of amine hydrohalides 5 with potassium thiocyanate has been developed. This approach tolerates sterically bulky primary amine substrates (both chiral and achiral), and the products can usually be isolated by a simple filtration of the reaction mixture. This method is an especially attractive alternative for the synthesis of thioureas when the corresponding isothiocyanates are unavailable, or difficult to prepare. It is also worth noting that a wide variety of amine hydrohalides, which are used in this procedure, are commercially available.
- Herr,Kuhler,Meckler,Opalka
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p. 1569 - 1574
(2007/10/03)
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- Thiocarbamoylation of amine-containing compounds 4. Reactions of tetramethylthiuram disulfide with aliphatic amines
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Thiocarbamoylation of primary and secondary aliphatic amines with tetramethylthiuram disulfide in various solvents at different temperatures was studied. At 110 °C, the reactions with primary amines afforded mixed N,N-dimethyl-N′-alkyl(cycloalkyl)thiourea
- Van Boi, Luu
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p. 2294 - 2298
(2007/10/03)
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- A convenient route to cyanoguanidines
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A facile and versatile method for the preparation of cyanoguanidines 7 from amines 3 and isothiocyanates 4 via a methylation, cyanamide-treatment sequence is described.
- Novak, Lajos,Hanania, Michel,Kovacs, Peter,Kovacs, Csilla Erika,Kolonits, Pal,Szantay, Csaba
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p. 1757 - 1766
(2007/10/03)
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- New syntheses of indole phytoalexins and related compounds
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Synthesis of indole phytoalexins brassinin, brassitin, cyclobrassinin and related compounds via 3-aminomethylindole and its 1-substituted derivatives obtained by nickel boride catalyzed reduction of corresponding aldoximes with sodium borohydride and via [1-(t-butoxycarbonyl)-indol-3-yl]methyl isothiocyanate, the first stable derivative of indol-3-ylmethyl isothiocyanate is described. Antifungal activity of the prepared compounds was examined by using the fungus Bipolaris leersiae by t.l.c. bioassay and quantitative screening was carried out with the selected compounds.
- Kutschy, Peter,Dzurilla, Milan,Takasugi, Mitsuo,Toeroek, Marcel,Achbergerova, Ingrid,Homzova, Renata,Racova, Maria
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p. 3549 - 3566
(2007/10/03)
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- A Concise and Convenient Method for the Synthesis of Pure Substituted Thioureas
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Zinc dialkyldithiocarbamates offer excellent substrates for pure thioureas required for the ntifungal and X-ray crystallographic studies.
- Ramadas, K.,Janarthanan, N.
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p. 1101 - 1108
(2007/10/03)
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- Lac sulfur assisted synthesis of symmetrical thioureas
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This work presents a short and attractive method to synthesise a variety of 1,3-disubstituted symmetrical thioureas in high yields.
- Ramadas,Janarthanan,Velmathi
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p. 2255 - 2260
(2007/10/03)
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- Reaction of Carbodiimides with Phosphorothioic, Phosphorodithioic, and Phosphoroselenoic Acids: Products, Intermediates, and Steps
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The reaction of the title acids with dicyclohexylcarbodiimide (DDC) used in a 2:1 ratio was found to give a complex mixture of products consisting of thio(seleno)pyrophosphates, thiolo(selenolo)phosphates, thiono(selenono)phosphates, dicyclohexylthiourea (DCTU), and a polymeric alkyl metaphosphate.When both reaction components are mixed in a 1:1 ratio, N-phosphoryl-N,N'-dicyclohexylthio(seleno)ureas (B) were formed.The formation of equimolar adducts (B) was also observed with other dialkyl- and diarylcarbodiimides.The spectral properties (especially the value of 3JP-H) and reactivity of these adducts are strongly dependent on their conformation.The distinct conformational differences between the adducts B derived from DCC and diisopropylcarbodiimide (DiPC) and those obtained from dibenzylcarbodiimide (DBC) and diarylcarbodiimides were revealed by X-ray analysis of the selected N-phosphorylthioureas.By means of low temperature FT 31P NMR spectra it was demonstrated that the adducts (B) arise from the first formed unstable S(Se)-phosphorylisothio(seleno)ureas (A) as a result of S(Se)->N-phosphoryl migration.The differences in ability of the phosphoryl group to undergo S(Se)->N and O->N 1,3-shifts are briefly described.N-Phosphorylthio(seleno)ureas (B) obtained from DCC and DiPC, in contrast to those prepared from DBC and diarylcarbodiimides, reacted with a second thio(seleno)acid molecule.Crossover experiments and the use of O,O-diethyl phosphorothioate containing 35S-labeled sulfur showed that the adducts (B) are in equilibrium with their unstable isomers (A), the latter being active phosphorylating agents.The formation of the final reaction products was rationalized in terms of the threedirectional attack of the thioacid anion at the phosphorus, alkoxy carbon, and central carbon atoms of the protonated adduct (A).
- Mikolajczyk, Marian,Kielbasinski, Piotr,Basinski, Wlodzimierz
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p. 899 - 908
(2007/10/02)
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- Reaction of 2,4-Bis-(4-methoxyphenyl)-1,3,2,4-dithiadiphosphetane 2,4-Disulphide with Urea Derivatives, Carbamates and Thiocarbamates
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Thiation of a series of urea derivatives, carbamates and thiocarbamates has been carried out by treatment with 2,4-bis-(4-methoxyphenyl)-1,3,2,4-dithiadiphosphetane 2,4-disulphide (1) under different conditions.Some of the products have been screened for their bactericidal activity.
- El-Barbary, A. A.,Lawesson, S. O.
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p. 655 - 657
(2007/10/02)
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- Applications of Phase Transfer Catalysis, 26. - Thioureas by Three-Component Reactions of Amines, Carbon Tetrachloride, and Sulfide Ions
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The title reactions proceed exothermically in the presence of a phase transfer catalyst.Thiophosgene is an intermediate in this conversion, and its phase transfer catalytic transformation into carbon disulfide and trithiocarbonate can be demonstrated.Perchloromethanethiol/sodium sulfide and a PT catalyst yield thiophosgene too.Activated vicinal dibromides were debrominated by Na2S/catalyst.
- Broda, Witold,Dehmlow, Eckehard V.
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p. 1839 - 1843
(2007/10/02)
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- Preparation and Some Reactions of Bis(thioacyl) Sulfides
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Reaction of dithioic acids with dicyclohexylcarbodiimide has been found to give the corresponding bis(thioacyl) sulfides 1 in good yield, which are very useful thioacylating reagents under mild reaction conditions.Most of the aromatic thioanhydrides (1, R = aromatic) are fairly stable green crystals at room temperature, but the aliphatic ones (1, R = aliphatic) are unstable purple oils which dimerize at room temperature to give the dithietanes 5.The reactions with nucleophiles are discussed.
- Kato, Shinzi,Shibahashi, Hiroshi,Katada, Tomonori,Takagi, Takashi,Noda, Ippei,et al.
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p. 1229 - 1244
(2007/10/02)
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- Cephalosporin displacement reaction
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The present invention is directed to a process for the displacement of the acetoxy group of a cephalosporanic acid by a sulfur nucleophile, in an organic solvent and under essentially anhydrous conditions.
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- Thiazolidine derivatives
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The invention relates to thiazolidine derivatives having in 4-position a hydroxy group and a 3'-sulphamyl-phenyl substituent the phenyl ring of which is di-substituted by halogen or methyl, in 2 position an imino group and in 1-position an aliphatic or cycloaliphatic substituent. Said thiazolidines have diuretic activity. The invention also relates to a process for the manufacture of said compounds.
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- Thiazolo[3,4-b]isoquinoline derivatives and pharmaceutical compositions containing them
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Thiazolo[3,4-b]isoquinoline derivatives of the general formula: STR1 wherein A represents 3-pyridyl, 4-pyridyl or 5-isoquinolyl and, when A represents 3-pyridyl, X1 represents hydrogen, halogen, dimethylamino or cyano, X2 represents
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