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Information × Registration Number 0215U009337, 0115U001979 , R & D reports Title 4-Thiazolidinone derivatives and related heterocyclic systems as prototypes of potential antitrypanosomal drugs popup.stage_title Head Lesyk Roman Bogdanovych, Доктор фармацевтичних наук Registration Date 25-12-2015 Organization Danylo Halytsky Lviv National Medical University popup.description2 The synthetic protocols for the formation of new 4-thiazolidonones and related heterocycles were worked out. The development of the reactions' conditions led to the obtaining of the new sub-library of 2-hydrazono-4-thiazolidinones and thiopyrano[2,3-d]thiazoles. New derivatives of 2- (heteryliden)hydrazono-4-thiazolidinones were obtained under [2+3]-cyclocondensation of heterylthiosemicarbazones with maleic anhydride, arylmaleyineimides, gamma-bromo- -butyrolaktone and oxoxmpounds. It is shown that 5- (ortho-hydroxyphenylmetylidene)substituted 4-thiazolidinethiones are effective agents for the multicomponent tandem processes involving hetero-Diels-Alder reaction. It opens new possibilities for the synthesis of polyfused heterocycles based on thiopyrano[2,3-d]tiazole "matrix". It was established that the interaction of 5-(2-hydroxyphenylmetylidene)-4-thioxo-2-thiazolidinones and unsaturated aldehydes belongs to the tandem hetero-Diels-Alder reaction. The latter lead to the formation of the semiacetals and allows to obtain new rel-(5aR, 6R, 11bS)- and rel-(5S,5aR,6R,11bS)-6-hydroxy-3,5a,6,11b-tetrahydro-2Н,5Н-chromeno[4',3':4,5]thiopyrano[2,3-d]thiazol-2-ones. The reactions are regi- and diastereoselective. A new variant of tandem reaction of acylation-hetero-Diels-Alder via interaction of 5- (ortho-hydroxyphenylmethyliden)isorhodanines and gamma crotonolactone was discovered. This is efficient direction for the formation of new rel-(5R,5aR,11bS)-5-hydroxymethyl-3,5,5a,11b-tetrahydro-2Н,5Н-chromeno[4',3':4,5]thiopyrano[2,3-d]thiazol-2,6-diones. The structure of the synthesized compounds and chemical research interpretation were confirmed by NMR spectroscopy and X-ray analysis.5481 Product Description popup.authors Камінський Д.В. Крищишин А.П. Лесик Р.Б. Лозинський А.В. Нєктєгаєв І.О. popup.nrat_date 2020-04-02 Close