- Mild and Chemoselective Thioacylation of Amines Enabled by the Nucleophilic Activation of Elemental Sulfur
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A mild and chemoselective method for the thioacylation of amines using α-keto acids and elemental sulfur has been developed. The key to the success of this transformation is the nucleophilic activation of elemental sulfur by thiols such as 1-dodecanethiol
- Saito, Masato,Murakami, Sho,Nanjo, Takeshi,Kobayashi, Yusuke,Takemoto, Yoshiji
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supporting information
p. 8130 - 8135
(2020/05/20)
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- Method for synthesizing 3-aryl thiopropionamide derivative
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The invention relates to a method for synthesizing a 3-aryl thiopropionamide derivative. The method comprises the following step: by taking an aryl allylene derivative as a substrate, an alkali as a promoter and elemental sulfur as a sulfur source, perfor
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Paragraph 0029
(2020/01/08)
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- Rapid and efficient protocol for Willgerodt–Kindler’s thioacetamides catalyzed by sulfated polyborate
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Abstract: A simple and efficient method for the synthesis of one-pot, three-component thioacetamides via Willgerodt–Kindler reaction was developed using a sulfated polyborate catalyst. The method described the reaction of ketones, sulfur, and secondary am
- Rekunge, Deelip S.,Khatri, Chetan K.,Chaturbhuj, Ganesh U.
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p. 2091 - 2095
(2017/10/06)
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- Aqueous Compatible Protocol to Both Alkyl and Aryl Thioamide Synthesis
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An efficient aqueous synthesis of thioamides through aldehydes, sodium sulfide, and N-substituted formamides has been developed. Both alkyl and aryl aldehydes are amenable to this protocol. N-Substituted formamides are essential for this transformation. Readily available inorganic salt (sodium sulfide) serves as the sulfur source in water, which makes this method much more practical and efficient. Furthermore, the late-stage modification of bioactive molecules and derivatives through this protocol has been established.
- Wei, Jianpeng,Li, Yiming,Jiang, Xuefeng
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supporting information
p. 340 - 343
(2016/02/03)
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- Sulfated tungstate: A green catalyst for synthesis of thiomorpholides via Willgerodt-Kindler reaction
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Use of sulfated tungstate as an efficient, green and reusable catalyst for preparation of thiomorpholides via Willgerodt-Kindler reaction pathway is presented. The reaction proceeds under solvent free condition. The advantages of this method are high yiel
- Salim, Suresh D.,Pathare, Sagar P.,Akamanchi, Krishnacharya G.
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experimental part
p. 78 - 81
(2012/06/04)
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- Microwave-assisted rapid hydrolysis and preparation of thioamides by Willgerodt-Kindler reaction
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Aldehydes and aryl alkyl ketones were efficiently transformed to thioamides with the same number of carbon atoms via Willgerodt-Kindler reaction under microwave irradiation in solvent-free conditions. The thioamides obtained were hydrolyzed to corresponding carboxylic acids with microwave dielectric heating in one minute. Both reactions are very fast and the yields are excellent.
- Matloubi Moghaddam,Ghaffarzadeh
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p. 317 - 321
(2007/10/03)
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- The rapid synthesis of thiomorpholides by Willgerodt-Kindler reaction under microwave heating
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The Willgerodt-Kindler reaction of several aryl alkyl ketones with sulfur and morpholine under solvent-free conditions was performed in a domestic microwave oven. Good yields were attained within a very short reaction time (between 3.5-6 min.).
- Nooshabadi, Masoud,Aghapoor, Kioumars,Darabi, Hossein Reza,Mojtahedi, Mohammad Majid
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p. 7549 - 7552
(2007/10/03)
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- Non-staining and slightly-staining antiozonants
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There is disclosed compounds having, within their structural formulae, a trivalent moiety: STR1 which exhibit antiozonant activity when added to rubber compositions at antiozonant effective levels and which exhibit synergistic antiozonant activity when used with conventional antiozonants in rubber compositions. There is also disclosed novel compounds which can be used as antiozonants.
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- The Willgerodt-Kindler Reactions. 6. Isomerization of the Carbonyl Group in Alkanones and Cycloalkanones
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The most unusual feature of the Willgerodt-Kindler Reactions is the facile isomerization of the carbonyl function along a chain of unbranched methylene groups, or around a cycloaliphatic ring containing several connected methylene groups.We have demonstrated that the first step in the Kindler process is the formation of enamines by reaction of the carbonyl function with secondary aliphatic amines, followed by reaction of the enamine with certain sulfur-amine catalysts to form reactive heterocyclic sulfur intermediates that facilitate the elimination-readdition of the amines reversibly along the chain.It was shown that compounds of the type R2N-S-S-NR2 are effective catalysts but not compounds of the type R2N-S-NR2.Some cyclohexanone derivatives undergo aromatization, with anomalous results in certain cases.
- Carmack, Marvin,Behforouz, Mohammad,Berchtold, Glenn A.,Berkowitz, Samuel M.,Wiesler, Donald,Barone, Ralph
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p. 1305 - 1318
(2007/10/02)
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- Substituted 1,3,4-Thiadiazoles with Anticonvulsant Activity. 2. Aminoalkyl Derivatives
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This paper describes the synthesis and pharmacological evaluation of a number of substituted 1,3,4-thiadiazoles.The first member of the series, 2-(aminomethyl)-5-(2-biphenylyl)-1,3,4-thiadiazole (7) was found to possess potent anticonvulsant properties in rats and mice and compared favorably with the standard anticonvulsant drugs phenytoin, phenobarbital, and carbamazepine in a number of test situations.The potency of compound 7 was maintained on alkylation of the side-chain nitrogen atom; however, aryl substitution or chain lengthening caused a drop in potency.Replacement of the 2-biphenylyl group by phenyl or benzyl also lead to inactive compounds.
- Stillings, Michael R.,Welbourn, Anthony P.,Walter, Donald S.
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p. 2280 - 2284
(2007/10/02)
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