75052-60-7Relevant academic research and scientific papers
Synthesis of various fused heterocyclic rings from thiazolopyridine and their pharmacological and antimicrobial evaluations
Balamon, Mina G.,Mahmoud, Naglaa F. H.
, (2020)
Various fused-heterocyclic-derivatives containing thiazolopyridine moieties has been synthesized by allowing 5-aminothiazolo[3,2-a]pyridine derivative 1 to undergo annulations reactions with different reagents under different-reaction conditions. The biological assessment of compounds 2, 11, 14, 15, and 19 showed remarkable antimicrobial activities. In addition, selected derivatives of the products were screened for their anticancer activities against two tumor cell lines using MTT assay and the results showed that some of these compounds have potent cytotoxic effect, as concluded from their IC50 values. Meanwhile, compounds 3a, 7 have exhibited very strong potency as anticancer candidates. Thiazolopyridine structures have been confirmed as a useful lead compounds for the development of new anticancer agents. Molecular docking showed that,-some of the synthesized compounds more suitable inhibitor against-ALR2 with farther alteration in future.
Method and catalyst for preparing thiazolo [3, 2-alpha] pyridine derivatives
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Paragraph 0055; 0056; 0057, (2017/07/20)
The invention discloses a method and a catalyst for preparing thiazolo [3, 2-alpha] pyridine derivatives, and belongs to the technical field of organic chemical industry. Magnetic material loaded alkaline ionic liquid is used as the catalyst, a molar ratio of aromatic aldehyde to active methylene compounds to methyl thioglycolate in preparation reaction is 2:(2-2.5):1, the molar weight, which is computed on the basis of alkaline ionic liquid on load, of the magnetic material loaded alkaline ionic liquid, which is the catalyst, is 8-12% of the molar weight of the methyl thioglycolate, and the reflux reaction time is 17-67 min. Compared with other preparation methods, the method and the catalyst have the advantages that the catalyst is low in loss during recycling and is high in recyclable times and product selectivity, integral preparation procedures are simple, convenient and economical, and accordingly industrial large-scale production can be facilitated.
One-pot synthesis of thiazolo[3,2-α]pyridine derivatives catalysed by ionic liquids
Chen, Hai-Liang,Guo, Hong-Yun
experimental part, p. 162 - 165 (2012/09/22)
A green method for the synthesis of thiazolo[3,2-α]pyridine derivatives via the coupling of malononitrile, an aryl aldehyde and methyl thioglycolate in an ionic liquid has been developed. The advantages of this protocol are that it is non-toxic, no by-products are formed, short reaction times are required and high yields are obtained. Thiazolo [3,2-a]pyridines have important biological and medical applications.
Synthesis of ethoxyphthalimido derivatized thiazolodihydropyridines assembled with pyrazole and isoxazole systems from common intermediate chalcone and evaluation of their antibacterial activity
Pemawat, Gangotri,Talesara, Ganpat L.
experimental part, p. 1173 - 1180 (2011/10/13)
Condensation of aromatic aldehydes, malononitrile and thioglycolic acid gives 5-amino-3-oxo-7-substitutedphenyl-2-substitutedarylidene-2,3-dihydro-7H- [1,3]thiazolo[3,2-a] pyridine-6,8-dicarbonitrile 1a-e. This acts as key intermediate for two series of f
THE REACTION OF THIOGLYCOLIC ACID WITH α,β-UNSATURATED NITRILES: A NEW ROUTE FOR THE SYNTHESIS OF THIAZOLOPYRIDINES
Elnagdi, Mohamed Hilmy,Elmoghayar, Mohamed Rifat Hamza,Elghandour, Ahmed Hafez Hussein,Sadek, Kamal Usef
, p. 745 - 751 (2007/10/02)
The reaction of cinnamonitriles with thioglycolic acid in the presence of a basic catalyst affords thiazolopyridine derivatives.
Activated Nitriles in Heterocyclic Synthesis: The Reaction of Substituted Cinnamonitriles with 2-Functionally Substituted Methyl-2-thiazolin-4-one Derivatives
Sadek, Kamal Usef,Hafez, Ebtisam Abdel Aziz,Mourad, Abo-Elfetouh E.,Elnagdi, Mohamed Hilmy
, p. 824 - 828 (2007/10/02)
A variety of thiazolopyridine and 3-(2-thiazolin-2-yl)pyridine derivatives were synthesised via the reaction of arylsubstituted cinnamonitrile derivatives with 2-functionally substituted 2-thiazolin-4-one derivatives.Thiazolopyridines were a
