| Summary: | The hetero-Diels–Alder reaction is the main synthetic tool for obtaining pharmacological agents with a thiopyrano[2,3-<i>d</i>]thiazole motif. In the present work, an efficient method for the synthesis of pyrazoline-containing thiopyrano[2,3-<i>d</i>]thiazole is described. The pyrazoline-bearing dienophile was proposed and used as effective building block for the synthesis of the title compound. The structure of the synthesized <i>rel</i>-2-[4-chloro-2-[(5<i>R</i>,6<i>R</i>,7<i>S</i>)-6-[5-(4-methoxyphenyl)-3-(2-naphthyl)-3,4-dihydropyrazole-2-carbonyl]-5-methyl-2-oxo-3,5,6,7-tetrahydrothiopyrano[2,3-<i>d</i>]thiazol-7-yl]phenoxy]acetic acid (<b>3</b>) was confirmed by <sup>1</sup>H, <sup>13</sup>C, 2D NMR, and LC-MS spectra. Anticancer activity in “60 lines screening” (NCI DTP protocol) was studied in vitro for the title compound.
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