Application of Tsunoda reagent to the convenient synthesis of drug-like pyrazoles |
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Authors: | Arash Mosallanejad Olivier Lorthioir |
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Affiliation: | 1. Medicinal Chemistry, Oncology, IMED Biotech Unit, AstraZeneca, Cambridge CB4 0WG, UK |
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Abstract: | The versatility of the under-utilised (cyanomethylene)tributylphosphorane (CMBP, Tsunoda reagent) was demonstrated on two occasions in a drug discovery context. Firstly, the high reactivity of the phosphorane allowed the alkylation of a weakly acidic pyrazole when standard Mitsunobu conditions were unsuccessful. Secondly, the clean reaction profile generally obtained using CMBP allowed the direct use of the crude mixture in a subsequent Suzuki cross coupling. This reagent has utility when isolation of the Mitsunobu reaction product (e.g. containing a boronate) is not desirable. |
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Keywords: | Pyrazole synthesis Mitsunobu reaction Tsunoda reagent (Cyanomethylene)tributylphosphorane Microwave-assisted synthesis |
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