78950-30-8Relevant academic research and scientific papers
A efficient protocol for the synthesis of thioamides in [DBUH][OAc] at room temperature
Cao, Xian-Ting,Qiao, Li,Zheng, Hui,Yang, Hui-Yong,Zhang, Peng-Fei
, p. 170 - 175 (2018/01/17)
A novel, simple and eco-friendly method to synthesize thioamides from aryl nitriles and sodium sulfide (Na2S·9H2O) catalyzed by 1,8-diazabicyclo[5,4,0]undec-7-enium acetate ([DBUH][OAc]) ionic liquid (IL) at room temperature was developed in this paper. In this reaction, readily available inorganic salt (Na2S·9H2O) serves as the sulfur source, and various functional groups of aryl nitriles were well tolerated at room temperature. In addition, the products were easily separated from the IL which could be reused at least five times without considerable loss of its activity and applied in the green, concise synthesis of ethionamide.
Optimizing thiadiazole analogues of resveratrol versus three chemopreventive targets
Mayhoub, Abdelrahman S.,Marler, Laura,Kondratyuk, Tamara P.,Park, Eun-Jung,Pezzuto, John M.,Cushman, Mark
experimental part, p. 510 - 520 (2012/03/10)
Chemoprevention is an approach to decrease cancer morbidity and mortality through inhibition of carcinogenesis and prevention of disease progression. Although the trans stilbene derivative resveratrol has chemopreventive properties, its action is compromised by weak non-specific effects on many biological targets. Replacement of the stilbene ethylenic bridge of resveratrol with a 1,2,4-thiadiazole heterocycle and modification of the substituents on the two aromatic rings afforded potential chemopreventive agents with enhanced potencies and selectivities when evaluated as inhibitors of aromatase and NF-κB and inducers of quinone reductase 1 (QR1).
Heterocycle-bridged and conformationally constrained retinoids: Synthesis of 4-(7,8,9,10-Tetrahydro-7,7,10,10-tetramethyl-4H-benzo[6,7]chromeno-[4,3-d]thiazole-2-yl)benzoic acid
Lamei, Navid,Foroumadi, Alireza,Emami, Saeed,Amini, Mohsen,Shafiee, Abbas
experimental part, p. 1951 - 1956 (2011/06/19)
Retinoids are a class of synthetic and natural compounds structurally related to retinoic acid. In a search for discovery of a new class of heterocycle-bridged and conformationally constrained retinoids, here we report the synthesis of 4-(7,8,9,10-tetrahydro-7,7,10,10-tetramethyl-4H-benzo[6,7]chromeno[4,3-d]thiazole-2-yl)benzoic acid (10) starting from 5,6,7,8-tetrahydro-5,5,8,8-tetramethylnaphthalen-2-ol (13). Several approaches was attempted to obtain target compound 10. Structure elucidation of synthesized compounds has been made on the basis of elemental analysis and spectral data (1H NMR, IR and MS).
The BF3·OEt2-assisted conversion of nitriles into thioamides with Lawesson's reagent
Nagl, Michael,Panuschka, Claudia,Barta, Andrea,Schmid, Walther
experimental part, p. 4012 - 4018 (2009/05/27)
A method for the thiolysis of nitriles by applying Lawesson's reagent and facilitated by the addition of boron trifluoride-diethyl ether complex is reported. The method opens an easy access to primary thioamides. Aromatic, benzylic, and aliphatic nitriles were converted into the corresponding thioamides in high to quantitative yields (even in unfavorable cases, e.g., ortho-substitut-ed benzonitriles). The reaction was performed in 1,2-dimethoxyethane-tetrahydrofuran or toluene-diethyl ether solvent mixtures at 20-50°C, and exhibited considerable selectivity in the case of multifunctional nitrile substrates, such as cyanomethyl N-acetylphenylalaninate, benzoylacetonitrile, 4-cyanobenzamide, 4-acetylbenzonitrile, or pent-3-enenitrile. Georg Thieme Verlag Stuttgart.
FACTOR XA INHIBITORS
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Page/Page column 216-217, (2008/06/13)
The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
