Herein, we report an efficient strategy to synthesize functionalized 1,3-thiazoles using alkyl 2-amino-2-thioxoacetates. Thioamides, the synthetic precursors, react effortlessly with electrophilic reagents and are transformed into a series of phenyl-, methyl-, and acyl-substituted thiazoles with high functionalization at the 2 position through sequential C-S/C-N bond formation. Rapid reaction times under metal-free mild conditions is a noteworthy feature of the reported protocol.
View Article and Find Full Text PDFJ Org Chem
August 2023
An acid-catalyzed regioselective cyclization reaction of 2,5-disubstituted-1,3,4-thiadiazoles and 1,3,4-oxadiazoles has been developed. The synthetic precursors alkyl 2-(methylthio)-2-thioxoacetates/alkyl 2-amino-2-thioxoacetates react efficiently with acyl hydrazides, which transformed into a series of dehydrative and desulfurative products with employment of -TSA and AcOH through a regioselective cyclization process. The alkyl 2-amino-2-thioxoacetate pathway generates excellent yield among the mentioned procedures.
View Article and Find Full Text PDFJ Biomol Struct Dyn
December 2023
Two novel thiazole derivatives, () and () have been synthesized, and their crystal structures determined by X-ray diffraction. To rationalize their structure, reactivity and druggability, we have performed a series of separate, but complementary studies. Hirshfeld surface and 2D-fingerprint plots were first scrutinized to qualitatively unveil all the intermolecular interactions that ensure their crystal packing.
View Article and Find Full Text PDFPersonnel protective equipment, N95 masks, and filtering facepiece respirators such as goggles, face shields, played a very important rolein the safety of bothvirus-affected persons and as well as medical staff, health workers. As the coronavirus (Covid-19) was increasing exponentially worldwide, healthcare has been the demand for this basic equipment especiallyface protection shields have critical issues. There has been an effort to find out the different ways to conserve PPE kits, to use after the sterilization process.
View Article and Find Full Text PDFThe regioselective synthesis of 2-(methylthio)--aryl/alkylthiazole-5-carboxamides and ethyl-5-(aryl/alkyl carbamoyl)thiazole-4-carboxylates was carried out the base-induced cyclization of methyl-2-oxo-2-(amino)ethanedithioates with TosMIC and ethyl isocyanoacetate, respectively, with high yields. The regioisomeric products were confirmed based on X-ray diffraction studies. An advantage of the present method is the wide-ranging isocyanide reactivity compared to earlier protocols, while the catalyst-free nature and rapid reaction times are noteworthy features.
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