A library of novel 4-[4-(4-nitrophenoxy)phenyl]-5-substituted-2H-1,2,4-triazole-3-thiones containing different substituents at the 5-position is synthesized. The mechanochemical treatment is followed to synthesize target compounds 8 (ap), and the yields are compared by both the grinding method and the conventional method. The structure of the intermediate, isothiocyanato-4-(4-nitrophenoxy)benzene 6, is analyzed by single crystal X-ray studies. The title compounds are characterized by spectral and elemental analyses and further evaluated for their efficacy as anthelmintics in vitro. Compounds 8c, 8j, 8k, 8l, and 8m exhibit significant anthelmintic activity.

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The paper describes industrially scalable synthesis and single crystal studies of 3-cyclopropyl-3,4-dihydroquinazolin-2(1H)-one 4, a versatile intermediate in the synthesis of number of biologically active compounds. The target compound has been characterized by LC-MS, 1 H NMR and IR. The crystal structure analysis shows that the title compound crystallizes in monoclinic class under the space group P 1 21/n 1 with cell parameters, a = 10.273(2) Å, b = 8.3227(19) Å, c = 11.623(3) Å, β = 104.980(3)°, V = 960.0(4) Å 3 and Z=4.