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[摘要]：A general and efficient method for the microwave-assisted formation of the C-P bond was developed. Using a prevalent palladium catalyst, Pd(PPh3)4, a quant. cross-coupling of various H-phosphonate diesters with aryl and vinyl halides was achieved in less than 10 min. Thus, microwave-assisted and Pd(PPh3)4-catalyzed cross-coupling of PhI with (EtO)2P(O)H in the presence of Cs2CO3 in THF at 120?in 10 min. gave 90% PhP(O)(OEt)2. The reactions occurred with retention of configuration at the phosphorus center and in the vinyl moiety. Using this protocol, several C-phosphonates, including those bearing nucleoside and cholesteryl moieties, were prepd. in high yields. |
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