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

Ravi Kumar Sadineni; Rajesh Kumar Rapolu; V. V. N. K. V. Prasada RajuN. SrinivasuSireesha MalladiNaveen Mulakayala

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

机译：lenvatinib使用的合成的新方法4？制药盐

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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.

机译：4-Nitrophenyl cyclopropylcarbamate部署一种新型合成纤维的合成抗癌药物lenvatinib。cyclopropylcarbamate是准备的反应的4-nitrophenyl氯甲酸酯和环丙基在乙腈胺在室温下。此外,lenvatinib合成反应4 - (4-amino-3-chlorophenoxy)7-methoxyquinoline-6-carboxamide与4-nitrophenyl cyclopropylcarbamate良好收益率。柠檬酸、磷酸、苹果酸和草酸盐lenvatinib中也发现了不错的收益。

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来源
《Chemical papers》 |2021年第4期|1475-1483|共9页
作者
Ravi Kumar Sadineni; Rajesh Kumar Rapolu; V. V. N. K. V. Prasada RajuN. SrinivasuSireesha MalladiNaveen Mulakayala;
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作者单位

SVAK Life Sciences, ALEAP Industrial Area, Pragathi Nagar, Hyderabad 500090, India;

Granules India Limited, R&D Center, Plot No. 56, Road No. 5, ALEAP Industrial Area, Pragathi Nagar, Hyderabad 5000072, India;

Division of Chemistry, Department of Sciences and Humanities, Vignan’s Foundation for Science, Technology and Research (VFSTR) (deemed to be) University, Vadlamudi, Guntur 522 213, India;

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原文格式 PDF
正文语种英语
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Lenvatinib; synthesis; Salts4-nitrophenyl;

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

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