Starting from epothilone A±D (1a±2b) obtained by large scale fermentation of the myxobacterium Sorangium cellulosum the thiazole side-chain was extensively modi®ed by substitution, oxidation and replacement. Metallation afforded the C-19 carbanion 4 which was quenched by various carbon and heteroatom electrophiles to give C-19 substituted epothilones 5. Thiazole N-oxides 9 were obtained by trea...

Condensation of 3-acetyl-8-ethoxycoumarin (3) with thiosemicarbazide gave ethylidenehydrazinecarbothioamide 5, which was transformed into the thiazolidin-4-one derivatives 6,7. Interaction of 3 with DMF/POCl(3) gave b-chloroacroline derivative 8. Treatment of 3 with malononitrile gave benzo[c]chromone and 2-aminobenzonitrile derivatives 9 and 10, respectively with respect to the reaction condit...

Thiazolo[5,4-d]thiazoles are valuable materials for a range of technical and biological applications. They used as chemosensors, electroluminescent materials, organic light-emitting diodes (OLEDs), in solar cells, live-cell imaging, etc., those applications π-extended thiazolo[5,4-d]thiazole derivatives particularly attractive. A convenient synthetic route to non-symmetrical thiazolo[5,4-d]thia...

Z-configurated isomers are kinetically preferred molecules. Compounds with Z-configuration contained in many natural products, biologically active compounds and as synthons for organic synthesis. Two series of new thiazole-based analogs were synthesized from appropriate starting materials hydrazinecarbothioamide derivatives (Z)-2a,b to be evaluated their inhibitory activity towards VEGFR-2. The...