A New Synthesis of Gefitinib
| Autor: | Tyler Kristufek, Taber S. Maskrey, Prasanth R. Nyalapatla, Peter Wipf, Matthew G. LaPorte |
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| Rok vydání: | 2018 |
| Předmět: | |
| Zdroj: | Synlett. 30:471-476 |
| ISSN: | 1437-2096 0936-5214 |
| Popis: | A four-step synthesis of the FDA-approved anticancer agent gefitinib was developed starting from 2,4-dichloro-6,7-dimethoxyquinazoline. Reaction temperatures were highly practical (0–55 °C), and chromatographic purifications were avoided. The ionic liquid trimethylammonium heptachlorodialuminate was used to monodemethylate the dimethoxyquinazoline core. In the final step, a selective dehalogenation was employed to provide gefitinib in 14% overall yield on a gram scale. |
| Databáze: | OpenAIRE |
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