PREPARATION OF beta-KETO-beta-ALKANOYLOXYPHOSPHONATES, PHOSPHINE OXIDES AND SULFIDES AND THEIR APPLICATION TO THE SYNTHESIS OF NOVEL PHOSPHORYL- AND THIOPHOSPHORYLPYRAZOLES

[摘要]：Two synthetic methods leading to beta-keto-beta-alkanoyloxyphosphonates, phosphine oxides and sulfides 2 are reported. The first method involves the reaction of beta-enaminoesters 1 with chlorophosphines and phosphites followed by oxidation or sulfurization and hydrolytic work-up. The second one utilizes the reaction of beta-enaminoesters 1 with diethylchlorophosphate and thiophosphate followed by acid hydrolysis. On reaction with hydrazine derivatives, compounds 2 give the corresponding phosphoryl- and thiophosphorylpyrazoles 3. The structures of all obtained products were confirmed by NMR (H-1, P-31, C-13) and IR spectroscopies, and by mass spectrometry.

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