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A new Heck reaction modification using ketone Mannich bases as enone precursors: parallel synthesis of anti-leishmanial chalcones |
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| Authors: | Reichwald Christina Shimony Orly Sacerdoti-Sierra Nina Jaffe Charles L Kunick Conrad |
| Affiliation: | 1. Technische Universität Braunschweig, Institut für Pharmazeutische Chemie, Beethovenstraße 55, 38106 Braunschweig, Germany;2. Department of Parasitology, Hebrew University-Hadassah Medical School, PO Box 12272, Jerusalem 91120, Israel |
| Abstract: | A new Heck-type reaction for the synthesis of chalcones has been established using Mannich bases as enone precursors. The novel reaction proceeds rapidly in air atmosphere under ligandless conditions and can be adapted for library synthesis in a parallel reactor station. Screening of the synthesized chalcones revealed N-{4-[(1E)-3-oxo-3-(3-pyridinyl)-1-propenyl]phenyl}benzamide (3f) to be a potent anti-leishmanial agent. |
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