Refernces
10.1016/j.tetlet.2008.01.038
The research focuses on the stereomeric studies of the oxidation and alkylation of 4-thiazolidinones, which are important cores in biologically active compounds with potential anti-inflammatory, antibacterial, anticancer activities, and other therapeutic properties. The study investigates diastereoselectivity in the oxidation of various 4-thiazolidinones to sulfoxides and sulfones, and the subsequent alkylation of these compounds with benzyl bromide. The experiments involved synthesizing different 4-thiazolidinones using aldehydes, benzylamine, and mercaptoacetic acid, followed by optimizing oxidation conditions to achieve high yields without overoxidation. The diastereoselectivity of the oxidation products was analyzed using HPLC and 1H NMR, with the best conditions found using AcOOH as the oxidant. The alkylation reactions were optimized using various bases, temperatures, and reaction times, with NaH found to be the most effective base. The stereoselectivity of the alkylation products was determined by HPLC and X-ray crystallography, revealing that the sulfoxide group influences the selectivity and that the substituent at carbon 5 and the sulfoxide are in a cis conformation.
10.1002/ardp.19873200311
The research focuses on the synthesis of novel thiazole, hydrazinopyrazole, and pyrazolo[5.1-c][1.2.4]triazine derivatives through the reaction of mercaptoacetic acid with 4-(cyanoacetyl)phenazone. The study investigates the behavior of the synthesized thiazolol towards diazonium salts, aldehydes, and hydrazines, and reports on the preparation of a pyrazolo[5.1-c][1.2.4]triazine derivative of phenazone by coupling diazotized 5-amino-3-phenazonylpyrazole with 2-phenacylthiazol-4-ol. The purpose of this research is to explore the chemical properties and potential pharmacological applications of phenazone derivatives, which are known for their anti-inflammatory, analgesic, sedative, and antipyretic properties. The chemicals used in the process include 4-(cyanoacetyl)phenazone, mercaptoacetic acid, diazonium salts, aldehydes, hydrazines, and various other reagents for the synthesis and characterization of the new compounds. The conclusions drawn from the research include the successful synthesis of several stable 2-thiazolin-4-ones and the establishment of their structures through spectroscopic data, as well as the observation of specific reactivity patterns towards different reagents.
10.1016/0039-128X(81)90038-6
The research focuses on the total synthesis of 12,15-bisthia-1,3,5(10),6,8,13(14)-gonahexaen-17-one (III), a heterocyclic steroid compound. The study aims to explore the influence of sulfur at position '12' of the steroid nucleus on biological activity, building on previous work on 3-deoxy-12-thiaequilenin and 12-thiaequilenin methyl ether. The synthesis involves a series of chemical reactions starting with 1-chloromethylnaphthalene (IV), which is treated with thioglycollic acid in sodium hydroxide to form l-naphthylmethyl-thioacetic acid (V). This compound is then cyclodehydrated with phosphorus pentoxide to yield 1-oxo-3-thia-1,2,3,4-tetrahydrophenanthrene (VI). Further reactions with thioglycollic acid and p-toluenesulfonic acid (PTS) lead to the formation of (3-thia-3,4-dihydrophenanthren-1-yl)thioacetic acid (VII), which is cyclodehydrated again to obtain the target compound (III).
10.1080/00304949809355295
The research focuses on developing a novel and efficient method for synthesizing phenylthioglycolic acids, which are important intermediates in the production of vat dyestuffs. The purpose of this study was to improve upon existing synthesis methods by achieving higher yields of these acids. The researchers utilized a two-step process involving the diazotization of substituted anilines followed by reaction with pyrrolidine to form aryltriazenes, which were then reacted with thioglycolic acid to yield the desired phenylthioglycolic acids. The study concluded that this new procedure resulted in higher yields compared to previously reported methods, demonstrating its effectiveness and potential for industrial applications.
10.1007/s11164-021-04558-9
This research focuses on the synthesis and application of a novel Fe3O4@THAM?CH2CH2?SCH2CO2H magnetic nanocatalyst for the efficient preparation of xanthenes and 3?aminoisoxazoles under green conditions. The purpose is to develop an environmentally friendly and efficient catalytic system that can be easily recovered and reused. The key chemicals used include FeCl3·6H2O, FeCl2·4H2O for synthesizing the Fe3O4 core, tris(hydroxymethyl)aminomethane (THAM) for coating, and thioglycolic acid for functionalization. The nanocatalyst was characterized using various analytical techniques such as FT-IR, TEM, VSM, XRD, TGA, and FE-SEM. The study concludes that this nanocatalyst can significantly reduce reaction times and improve yields while being easily recoverable by an external magnet for up to eight cycles without significant loss of activity. This method is advantageous due to its solvent-free conditions, mild reaction temperatures, and excellent yields, making it a sustainable and economic approach in line with green chemistry principles.
10.1016/j.bmcl.2009.04.125
The research aimed to develop new selective COX-2 inhibitors to treat inflammation and inflammation-associated disorders with reduced gastrointestinal toxicities compared to traditional NSAIDs. The study focused on synthesizing a new group of 3-alkyl-2-aryl-1,3-thiazinan-4-one derivatives with a methylsulfonyl pharmacophore and evaluating their COX-2 inhibitory activity. Key chemicals used in the synthesis included amines (such as benzylamine, phenethylamine, and cyclohexylamine), 4-methylthiobenzaldehyde, and thioglycolic acid. The most potent and selective COX-2 inhibitor identified was 3-benzyl-2-(4-methylsulfonylphenyl)-1,3-thiazinan-4-one (11a), with an IC50 of 0.06 μM and a selectivity index of 285.8. Molecular modeling suggested that the compound's potent and selective inhibitory activity was due to its specific interactions with the COX-2 active site. The study concluded that these derivatives could serve as promising candidates for the development of new anti-inflammatory drugs with fewer gastrointestinal side effects.
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