Phosphonylation of 3',4'-dihydroxy-L-phenylalanine (L-DOPA) has been achieved using inorganic diphosphonate (DP) in aqueous solution. The optimum condition for the phosphonylation of L-DOPA with DP is L-DOPA : DP = 1 : 10, pH 6 and 25 ºC. 3'-Hydroxy-4'-phosphonyl-L-phenylalanine and 3'-phosphonyl-4'-hydroxy-L-phenylalanine were synthesized with the total yield of more than 62 %. The phosphonylated products of L-DOPA were stable in neutral and acidic solution. The reaction mechanism of L-DOPA with DP was discussed.
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