Metal-Free Site-Selective Direct Oxidative Phosphorylation of Pyrazolones
A substrate-controlled site-selective phosphorylation of pyrazolin-5-ones has been established under metal-free direct oxidative coupling processes. A reaction between pyrazolones and secondary phosphonates in the presence of TBAI/TBHP combination could result in the N−P bond formation at N2 positio...
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| Format: | Article |
| Published: |
2023
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| Online Access: | https://repository.li.mahidol.ac.th/handle/123456789/84054 |
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| Institution: | Mahidol University |
| Summary: | A substrate-controlled site-selective phosphorylation of pyrazolin-5-ones has been established under metal-free direct oxidative coupling processes. A reaction between pyrazolones and secondary phosphonates in the presence of TBAI/TBHP combination could result in the N−P bond formation at N2 position. Meanwhile, the C−P bond coupling at C3 position could be obtained from a reaction of N2-substituted pyrazolone substrates with secondary phosphine oxides using Selectfluor. These chemo- and regioselective metal-free approaches proceed in fair to high yields under mild reaction conditions with good functional group compatibility. (Figure presented.). |
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