Abstract
4-Nitrophenyl cyclopropylcarbamate was deployed as a novel synthon for the synthesis of anticancer drug lenvatinib. 4-Nitrophenyl cyclopropylcarbamate was prepared by the reaction of 4-nitrophenyl chloroformate and cyclopropyl amine in acetonitrile at room temperature. Furthermore, lenvatinib was synthesized by reacting 4-(4-amino-3-chlorophenoxy)-7-methoxyquinoline-6-carboxamide with 4-nitrophenyl cyclopropylcarbamate in good yields. Apart from the synthesis of lenvatinib, citrate, phosphate, malate and oxalate salts of lenvatinib were also reported in good yields.
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We thank the management of Granules India Ltd. and management of Vignan's Foundation for Science, Technology and Research (VFSTR)
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Sadineni, R.K., Rapolu, R.K., Raju, V.V.N.K.V.P. et al. Novel method for the synthesis of lenvatinib using 4-nitrophenyl cyclopropylcarbamate and their pharmaceutical salts. Chem. Pap. 75, 1475–1483 (2021). https://doi.org/10.1007/s11696-020-01402-z
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DOI: https://doi.org/10.1007/s11696-020-01402-z