Spectral data of coumarin isoxazoline derivatives 11a-d. Spectral data of coumarin isoxazoline derivatives 12a-d.1 H NMR , 13 C NMR, Mass and Elemental analysis Spectra of compound 11a.1 H NMR , 13 C NMR, Mass and Elemental analysis Spectra of compound 12a.

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An improved and novel process for the synthesis of antiviral drug Darunavir using 4-(1,3-dioxoisoindolin-2-yl)benzene-1-sulphonyl chloride was described to eliminate the critical furan dimer impurity which will be formed during the process. The best reaction conditions were identified by evaluating the impurity profile and their formation during the synthesis. The optimization of the process was made to control the furan dimer impurity which was one of the critical parameters in the synthesis of darunavir. All the impurities formed during the synthesis were identified, synthesized and characterized.

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Background: A new series of quinazoline linked chalcone conjugates were synthesized and evaluated for their in vitro cytotoxicity. Methods: The quinazoline-chalcone derivatives (13a-r) have been prepared by the Claisen-Schmidt condensation of various substituted benzaldehydes (12a-r) with substituted l-(4-(3,4dihydroquinazolin-4-ylamino)phenyl)ethanone (11a-b) in the presence of aqueous NaOH. Three potential compounds 13f, 13g and 13h exhibited cytotoxicity against leukemia (GI 50 value of 1.07, 0.26 and 0.24 µM), Non-small lung (GI 50 values of 2.05,1.32 and 0.23 µM), colon (GI 50 values of 0.54, 0.34 and 0.34 µM) and breast (GI 50 values of 2.17, 1.84 and 0.22 µM) cell line, respectively. Results and Conclusion: Based on these biological results, it is evident that compound 13h has the potential to be considered for further detailed studies either alone or in combination with existing therapies as potential anticancer agents.