摘要 |
PROBLEM TO BE SOLVED: To provide a process for regioselective synthesis of diethylenetriaminepentaacetic acid (DTPA) derivatives.SOLUTION: The present invention provides a process for high yield regioselective synthesis of DTPA derivatives represented by formula (I), which eliminates the need for ion exchange chromatographic separation of intermediates, wherein A p-nitro-L-phenylalanine derivative is used as a raw material to convert it into isothiocyanate by thiophosgene after going through multistep process. Moreover, as this process yields a single regioisomer of the chelate, it provides for the regiospecific synthesis of desired chelates useful as radiolabeling agents. |