New Synthetic Process for Bosutinib
| Autor: | Chunping Zhu, Ziyang Kong, Jiao Wang, Xinfeng Ren, Yongjun Mao, Guoqing Zhu |
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| Rok vydání: | 2015 |
| Předmět: | |
| Zdroj: | Synthesis. 47:3133-3138 |
| ISSN: | 1437-210X 0039-7881 |
| DOI: | 10.1055/s-0035-1560471 |
| Popis: | A new and improved synthetic route to bosutinib is described on a hectogram scale. The key step is the intramolecular cyclization of a 3-(2-aminophenyl)-3-oxopropanenitrile with N,N-dimethylformamide dimethyl acetal to form the 3-cyano-4-hydroxyquinoline ring of 7-(3-chloropropoxy)-6-methoxy-4-oxo-1,4-dihydroquinoline-3-carbonitrile. A practical synthetic method to 2,4-dichloro-5-methoxyaniline is also established. Bosutinib is obtained in 18.0% yield over nine steps from acetovanillone with 98.9% purity (HPLC). |
| Databáze: | OpenAIRE |
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