- Gold(I)-catalyzed, one-pot, oxidative formation of 2,4-disubstituted thiazoles: Application to the synthesis of a pateamine-related macrodiolide
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Thiazoles are important heterocyclic motifs in many target molecules. Extension of a reported gold(I)-catalyzed oxidative coupling of alkynes and thioamides to the synthesis of functionalized thiazole-containing products is presented, including the compatibility of this reaction with ester, protected hydroxyl, alkene and thioether groups. The utility of this one-pot process is demonstrated in the preparation of the thiazole-containing macrodiolide of a simplified analogue of pateamine A.
- Xu, Tao,Cuyamendous, Claire,Brown, Sarah L.,Andreassend, Sarah K.,Cumming, Hemi,Evans, Gary B.,Teesdale-Spittle, Paul H.,Harvey, Joanne E.
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supporting information
(2021/05/04)
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- Microwave-assisted synthesis of potent PDE7 inhibitors containing a thienopyrimidin-4-amine scaffold
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A series of novel thienopyrimidin-4-amines have been synthesized and evaluated as phosphodiesterase (PDE) inhibitors. A rationale for the observed selectivity against PDE7 has been obtained from molecular modelling studies on the most active compounds. This journal is the Partner Organisations 2014.
- Sanchez, Ana I.,Meneses, Ricardo,Minguez, Jose M.,Nunez, Araceli,Castillo, Rafael R.,Filace, Fabiana,Burgos, Carolina,Vaquero, Juan J.,Alvarez-Builla, Julio,Cortes-Cabrera, Alvaro,Gago, Federico,Terricabras, Emma,Segarra, Victor
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p. 4233 - 4242
(2014/06/10)
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- A mild and versatile synthesis of thioamides
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Aliphatic and aromatic nitriles react with thioacetic acid in the presence of calcium hydride to give the corresponding thioamides in good to excellent yields. The examples studied include haloaryl nitriles in which the halogen is facile towards SNAr reactions under other conditions. Georg Thieme Verlag Stuttgart.
- Mahammed,Jayashankara,Premsai Rai,Mohana Raju,Arunachalam
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experimental part
p. 2338 - 2340
(2009/12/08)
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- NEW SUBSTITUTED 1,3-THIAZOLE DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF HAVING IMMUNOSUPPRESSION AND INFLAMMATION INHIBITORY ACITIVITY, INTERMEDIATE COMPOUNDS OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, A PROCESS FOR THE PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Disclosed relates to new substituted 1,3-thiazole derivatives or pharmaceutically acceptable salts thereof having immunosuppresion and inflammation inhibitory activity, intermediate compounds or pharmaceutically acceptable salts thereof, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The compound of the present invention having excellent TNF-α inhibitory activity and inflammation inhibitory activity can be effectively used in the prevention and treatment of TNF-α related diseases.
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Page/Page column 121-122
(2010/11/25)
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- Preparation of primary thioamides from nitriles using sodium hydrogen sulfide and diethylamine hydrochloride
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Primary thioamides are prepared in moderate to excellent yields by treating nitriles with sodium hydrogen sulfide and diethylamine hydrochloride in an appropriate solvent with mild heating. Copyright Taylor & Francis LLC.
- Boys, Mark L.,Downs, Victoria L.
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p. 295 - 298
(2007/10/03)
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- (+)-Cystothiazole G: Isolation and structural elucidation
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Palladium-catalyzed cyclization-methoxycarbonylation of (2R,3S)-3-methylpent-4-yne-1,2-diol (6) derived from (2R,3S)-epoxybutanoate 5 followed by methylation gave the tetrahydro-2-furylidene acetate (-)-7, which was converted to the left-half aldehyde (+)-3. A Wittig reaction between (+)-3 and the phosphoranylide derived from the bithiazole-type phosphonium iodide 4 using lithium bis(trimethylsilyl)amide afforded the (+)-cystothiazole G (2), whose spectral data were identical with those of the natural product (+)-2. Thus, the stereochemistry of cystothiazole G (2) was proved to be (4R,5S,6(E)).
- Akita, Hiroyuki,Sasaki, Takamitsu,Kato, Keisuke,Suzuki, Yoshihiro,Kondo, Keiko,Sakagami, Youji,Ojika, Makoto,Fudou, Ryosuke,Yamanaka, Shigeru
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p. 4735 - 4738
(2007/10/03)
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- Synthesis, characterization and blood cell labelling evaluation of new (99m)Tc nitrido radiopharmaceuticals with thioamide [R1C(=S)NHR2] derivatives
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The synthesis of a series of new (99m)Tc-thioamide complexes with the [Tc=N]2+ nitrido core, in which the thioamide ligand substituents were varied to include different lengths of atiphatic alkyl chains or a phenyl group is reported. TLC analysis shows that the complexes are neutral and lipophilic compounds. The (99m)Tc complexes have a low blood cell labelling efficiency in whole blood compared to the reference complex of dithiocarbamate (99m)TcN(Et(EtO)NCS2)2.
- Mevellec,Demaimay,Roucoux,Moisan,Noiret,Patin
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p. 863 - 869
(2007/10/03)
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- A new method for converting nitriles into primary thioamides by sodium trimethylsilanethiolate
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A new method was developed for converting nitriles into primary thioamides. Treatment of various nitriles 1 with 1.5-2.5 equivalents of sodium trimethylsilyl sulfide (sodium trimethylsilanethiolate) in 1,3-dimethyl-2-imidazolidinone at 20-35°C for 4-30 hours gave the corresponding thioamides 2 in 27-80% yield.
- Lin,Ku,Shiao
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p. 1219 - 1220
(2007/10/02)
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- Fluorophenoxyphenoxypropionates and derivatives thereof
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Novel intermediates useful in the preparation of fluorophenoxyphenoxypropionates and derivatives thereof which possess herbicidal activity selectively in the presence of broadleaf crops.
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- DIPHENYLPHOSPHINODITHIOIC ACID: A REAGENT FOR THE CONVERSION OF NITRILES TO THIOAMIDES
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Diphenylphosphinodithioic acid is a reagent useful for a sequence effecting the hydrolysis of nitriles under mild conditions.
- Benner, Steven A.
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p. 1851 - 1854
(2007/10/02)
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