- Preparation method of isothiocyano compound
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The invention discloses a preparation method of an isothiocyano compound. An ammonium thiocyanate, sodium thiocyanate or potassium thiocyanate water solution and a halide are used as raw materials, and an isothiocyano compound is synthesized under the action of a phase transfer catalyst. The requirements that the thiocyanate radical in each batch of reaction is excessive by 10% and the yield is high are met, the purpose that the concentration of thiocyanic acid in wastewater is very low is realized, complex wastewater treatment equipment and treatment operation are avoided, and environmental protection pressure is reduced. The preparation method is a green preparation method, and solves the problems of extremely difficult degradation and high biotoxicity of thiocyanate-containing wastewater in conventional isothiocyano compound production. The method is simple to operate and is suitable for industrial production.
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Paragraph 0013
(2019/10/29)
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- Double three bromo 1,3-di-pyridine salt-based propane and its preparation method, method of use, recovery method and application
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The invention discloses a double tribromo 1,3-bipyridine onium salt dimethylmethane, and a preparation method, an application method, a recovery method and application thereof. The preparation method comprises the following steps: dissolving 1,3-bipyridine onium salt dimethylmethane by using water, and then adding potassium bromide; adding potassium peroxymonosulfate sulfate compound brine solution to prepare a clear solution after dissolving potassium bromide, and then stirring and reacting at -10 to 0 DEG C until solid is separated out; separating out solid, so as to obtain the double tribromo 1,3-bipyridine onium salt dimethylmethane. The product can be used for preparing isothiocyanate, aromatic thiourea or acetanilide. The preparation method disclosed by the invention is mild in condition, and simple to operate the reaction process, and raw materials are easily available. The double tribromo 1,3-bipyridine onium salt dimethylmethane not only can be used as a brominating reagent, but also can be used as organic synthesis intermediates, meanwhile, the reaction efficiency is improved, and the double tribromo 1,3-bipyridine onium salt dimethylmethane is convenient to recover and can be recycled.
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Paragraph 0075; 0076; 0195; 0196
(2016/10/07)
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- Synthesis and biological activity of diisothiocyanate-derived mercapturic acids
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This Letter deals with new non-natural diisothiocyanates, their mercapturic acid derivatives - conjugated with N-acetylcysteine as well as their antiproliferative activity towards human colon cancer cell lines and their inhibitory potency towards histone deacetylase activity. The activity of analysed isothiocyanates is not significantly different than their N-acetylcysteine conjugates. In comparison to simple mono-isothiocyanate analogues, aliphatic diisothiocyanates and their conjugates are much more active than the simple presence of two isothiocyanate functionalities could indicate.
- Grzywa, Renata,Winiarski, ?ukasz,Psurski, Mateusz,Rudnicka, Agata,Wietrzyk, Joanna,Gajda, Tadeusz,Oleksyszyn, Józef
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supporting information
p. 667 - 671
(2016/01/09)
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- Synthesis and structure-activity relationships of aliphatic isothiocyanate analogs as antibiotic agents
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Isothiocyanates (ITCs) are one of the many classes of breakdown products of glucosinolates found in plants and exhibit biologic activity against various pathogens. In this work, aliphatic isothiocyanates were prepared and the antimicrobial activities against plant pathogenic fungi and bacteria were tested to understand the structure-activity relationships. The results indicated that longer-chain derivatives exert a steric inhibition on toxicity of ITCs against Rhizoctonia solani because of steric hindrance and the order of the eight aliphatic ITCs was ethyl > n-propyl > methyl > n-hexyl > n-octyl > n-butyl > n-heptyl > n-pentyl. Because the hydrophobicity of ITCs was enhanced by increasing alkyl chain length, the antibacterial activity of ITCs against Erwinia carotovora was moderately intense with an increase in hydrophobicity and the order was n-octyl > n-pentyl > n-heptyl > n-hexyl > n-propyl > n-butyl > methyl > ethyl. The present study revealed that some of the compounds exhibited promising antimicrobial activity and could be used as an acceptable alternative to the traditional synthetic fungicides for controlling R. solani and E. carotovora.
- Li, Deguang,Shu, Yanan,Li, Pingliang,Zhang, Wenbing,Ni, Hanwen,Cao, Yongsong
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p. 3119 - 3125
(2013/07/11)
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- A facile and new approach to synthesize 2-amino-4-(4-amoinophenyl)-1H-1,3- diazol-1-yl-alkylaminomethanethiones
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An "intellectual connection" approach to design a facile and new synthesis of suitably substituted 2-aminoimidazole-based precursors of expected anti-asthmatic agents through a benzidine type of rearrangement of 2-phenylazoimidazole and subsequent coupling of the product thus obtained with alkylisothiocyanates involving a degenerative operation, thereby improving the time frame of the overall synthetic sequence, is reported. The alkylisothiocyanates required in this synthetic sequence are prepared using a best combination of reported methods. The compounds reported here can be used to produce derivatives of other biological agents. Birkhaeuser 2007.
- Verma, Raman K.,Aggarwal, Monika,Bansal, Manisha,Kaur, Inder Preet
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p. 483 - 491
(2008/04/01)
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- Guanidino N-Substituted and N,N-Disubstituted Derivatives of the κ-Opioid Antagonist GNTI
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Derivatives of the highly selective κ-opioid receptor antagonist GNTI (2a) have been prepared. Binding and functional studies conducted on cloned human opioid receptors expressed in Chinese hamster ovarian (CHO) cells suggested that adding a benzyl or a substituted benzyl group to the guanidino moiety led, in general, to a retention of high κ-affinity and antagonist potency. Disubstitution of the guanidino moiety led to reduced κ-selectivity.
- Black, Shannon L.,Chauvignac, Cedric,Grundt, Peter,Miller, Carl N.,Wood, Susan,Traynor, John R.,Lewis, John W.,Husbands, Stephen M.
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p. 5505 - 5511
(2007/10/03)
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- Photoinduced and Thermal Isomerization Processes for Bis-Oxonols: Rotor Volume, Stereochemical and Viscosity Effects
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Four bis-oxonols have been synthesized which possess different alkyl substituents appended to the thiobarbiturate subunit.The nature of the alkyl substituent affects the photophysical properties of the dye in solution since it modulates the rate of rotation of the thiobarbiturate subunit around one of the double bonds in the connecting trimethine bridge.Rates of light-induced (trans to cis) and thermal (cis to trans) isomerization processes have been measured for one of the dyes in protic (i.e. alkanols) and aprotic solvents at various temperatures.These rates, together with activation energies derived from Arrhenius plots, are discussed in terms of the hydrogen bonding and stereochemical properties of the solvent.The thermal step is very sensitive to the stereochemistry of the solvent while the light-induced process is controlled mostly by the size of the rotor and the solvent viscosity.The overall effects may be explained, at least in a qualitative sense, in terms of the medium-enhanced barrier model.
- Benniston, Andrew C.,Harriman, Anthony
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p. 2627 - 2634
(2007/10/02)
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- A Method for the Simultaneous Preparation of Alkyl Isothiocyanates and Thiols
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Aus primaeren Alkylaminen wurden Ethyl-, Butyl-, Isobutyl- und n-Dodecyldithiocarbamate 2 hergestellt.Letztere lassen sich leicht zu den Isothiocyanaten 3 und Thiolen 4 pyrolisieren.Die Massenspektren der Ester sowie deren Pyrolyseprodukte wurden gemessen.
- Blotny, Grzegorz
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p. 1927 - 1932
(2007/10/02)
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- 5-Heterocyclic-1,2,3,6-tetrahydro-4(5H) pyrimidinone
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The compounds of this invention are 5-heterocyclic-1,2,3,6-tetrahydro-4(5H)-pyrimidinethiones which have pharmacological activity, in particular gastric acid secretion inhibitory activity, and 5-heterocyclic-1,2,3,6-tetrahydro-4(5H)-pyrimidinones which are intermediates in the preparation therefor.
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- 2-Alkoxy(and 2-alkoxyalkyl)-2-heterocyclic-thioacetamides for inhibiting gastric acid secretion
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The compounds are 2-alkoxy(and 2-alkoxyalkyl)-2-heterocyclic-thioacetamides which are inhibitors of gastric acid secretion.
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- 2-Alkoxy(and 2-amino)-3-amino-2-heterocyclic-thiopropanamides
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The compounds are 2-alkoxy(and 2-amino)-3-amino-2-heterocyclic-thiopropanamides, for example 2-methoxy-N-methyl-3-morpholino-2-(2-pyridyl)thiopropanamide, which are inhibitors of gastric acid secretion.
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- PHARMACOLOGICALLY ACTIVE THIOUREA AND UREA COMPOUNDS
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The compounds are substituted thioalkyl-, aminoalkyl-and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity.
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