- Sulfonic acid functionalized nano Γ-Al 2O 3: A new, efficient, and reusable catalyst for synthesis of thioamides
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Sulfonic acid functionalized nano γ-Al2O3 is easily prepared by the reaction of nano γ-Al2O3 with 1,3-propane sulfone. This reagent can be used as an eficient catalyst for the synthesis of thioamides. This new method consistently has the advantages of excellent yields and short reaction times. Further, the catalyst can be recovered for several times.
- Yin, Zhikui,Zheng, Bin,Ai, Fang
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p. 1412 - 1420
(2013/10/08)
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- Nano n -propylsulfonated magnetic γ-Fe2O3 as an efficient and reusable catalyst for the synthesis of thioamides
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One-pot three-component reactions of aldehydes, amines, and sulfur are carried out in the presence of nano n-propylsulfonated magnetic γ-Fe2O3 as a catalyst for the synthesis of biologically interesting thioamide derivatives. The value of this catalytic method lies in its mild reaction catalyst and conditions, good yields, and ease of handling.
- Yin, Zhikui,Zheng, Bin
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p. 527 - 531
(2013/10/21)
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- Synthesis of thioamides by catalyst-free three-component reactions in water
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Three-component reactions involving amines, aldehydes, and elemental sulfur powder are reported to afford thioamides in a simple one-pot procedure in the absence of a catalyst. A variety of thioamides can be obtained in good to excellent yields up to 88 %. Three-component reactions involving amines, aldehydes, and sulfur powder afford thioamides in a simple one-pot procedure. A variety of substituted thioamides are obtained in good to excellent yields up to 88 %. Copyright
- Xu, Hualong,Deng, Hang,Li, Zhengkai,Xiang, Haifeng,Zhou, Xiangge
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supporting information
p. 7054 - 7057
(2013/11/06)
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- Sulfated tungstate: An efficient catalyst for synthesis of thioamides via Kindler reaction
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New application of sulfated tungstate, a mildly acidic solid inorganic acid, as reusable heterogeneous catalyst for efficient Kindler reaction, a three component reactions of aldehydes, amines and sulfur, for synthesis of thioamides is discussed.
- Pathare, Sagar P.,Chaudhari, Pramod S.,Akamanchi, Krishnacharya G.
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experimental part
p. 125 - 129
(2012/07/03)
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- Efficient synthesis of thiobenzanilides by Willgerodt-Kindler reaction with base catalysts
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Willgerodt-Kindler reaction between anilines and benzaldehydes readily proceeded in the presence of catalytic amount of Na2S·9H 2O to give thiobenzanilides in moderate to good yields. The base catalyst was also available for preparation of primary thiobenzamide. Georg Thieme Verlag Stuttgart.
- Okamoto, Ken,Yamamoto, Takakazu,Kanbara, Takaki
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p. 2687 - 2690
(2008/02/11)
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- Structural Studies on Bioactive Compounds. 23. Synthesis of Polyhydroxylated 2-Phenylbenzothiazoles and a Comparison of Their Cytotoxicities and Pharmacological Properties with Genistein and Quercetin
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A series of polyhydroxylated 2-phenylbenzothiazoles 3 has been prepared by demethylation of the precursor methoxylated 2-phenylbenzothiazoles 9.The key step in the construction of the benzothiazole nucleus involves a Jacobson cyclization of methoxylated thiobenzanilides 8.The target compounds inhibit WiDr human colon tumor cells and MCF-7 human mammary tumor cells in vitro with IC50 values in the low micromolar range, but the activity against MCF-7 cells is not related to estrogen receptor-binding affinity.None of the compounds showed selective cytotoxicity againstAbelson virus-transformed ANN-1 cells encoded with the pp120gag-abl tyrosine kinase compared with the parental 3T3 line.Compounds were only marginally inhibitory to the EGF receptor-associated protein tyrosine kinase from a membrane preparation of A431 cells.The most active compound was 4,6-dihydroxy-2-(4-hydroxyphenyl)benzothiazole (3b) which has the same overall hydroxyl substitution pattern as genistein (1a).The compounds were weakly cytotoxic for an EGF receptor, overexpressing cell line HN5, but when tested for differential toxicity against the EGF receptor tyrosine kinase or the PDGF receptor tyrosine kinase in a standard mitogenesis assay utilizing human fibroplasts, no discrimination was observed.In this assay, the compounds inhibited DNA synthesis when added to cells during S phase.This suggests that inhibition could not be interpreted in terms of tyrosine kinase inactivation but more likely as a relatively broad specificity for the ATP-binding domain of other kinases such as thymidine kinase.
- Stevens, Malcolm F. G.,McCall, Carol J.,Lelieveld, Peter,Alexander, Peter,Richter, Audrey,Davies, Donna E.
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p. 1689 - 1695
(2007/10/02)
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- ANTIMYCOBACTERIAL THIOBENZANILIDES
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A group of 30 thiobenzanilides active against Mycobacterium kansasii have been synthesized and their 1H NMR and UV spectra and RM values (TLC on silica gel impregnated with methylsilicone oil) have been measured.From the correlation between the chemical shifts of the thioamide proton in the 1H NMR spectra and the Hammett constants it can be concluded that the substituents in both aromatic rings uniformly affect the electron density of the thioamide group.The antimycobacterial activity is probably connected with local molecular parameters and can be considered to be approximately additive with respect to both parts of the molecule.
- Waisser, Karel,Houngbedji, Nestor,Machacek, Milos,Sekera, Miroslav,Urban, Josef,Odlerova, Zelmira
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p. 307 - 316
(2007/10/02)
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- Synthesis and analgesic activity in 1,2,4-triazole series
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Derivatives of 1,2,4-triazole have been synthesized. Several methods of synthesis were used and the analgetic and antiinflammatory properties of the products obtained were studied. Structural requirements for analgetic activity were specified. Certain compounds show a high degree of analgetic activity. One of them, RU 39813, has been chosen for extended pharmacological study.
- Clemence,Joliveau-Maushart,Meier,et al.
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p. 257 - 266
(2007/10/02)
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