Novel method for the synthesis of lenvatinib using 4-nitrophenyl cyclopropylcarbamate and their pharmaceutical salts

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.

Automated summary

The compound 4-nitrophenyl cyclopropylcarbamate was used as a novel synthon for the synthesis of the anticancer drug lenvatinib, with good yields. In addition to lenvatinib, citrate, phosphate, malate, and oxalate salts of lenvatinib were also synthesized in good yields.