Preparation of 6-aminoquinazolin-4(3H)-ones via direct SNAr on the quinazoline ring |
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| Authors: | Bernard Barlaam Craig S Harris Jonathan Lecoq Ha Thi Hoang Nguyen |
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| Institution: | AstraZeneca, Oncology iMed, Centre de Recherches, Z.I. la Pompelle, BP1050, 51689 Reims Cedex 2, France |
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| Abstract: | The preparation of 6-aminoquinazolin-4(3H)-ones requires the use of platinum–metal group catalysis on the corresponding C-6-iodo or 6-bromo precursors. Herein, we report to our knowledge the first successful SNAr reaction directly at the unactivated C-6 position of the quinazolin-4(3H)-one nucleus. |
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