N-Hydroxysuccinimide → N-{4-[2-[bis(2-chloroethyl)amino]phenyl]butyroyl}-4-aminobutane-1,1-diphosphonic acid tetraethyl ester

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Reaction Steps

Following the procedure described in Example 1b), by reacting 4-[2-[bis(2-chloroethyl)amino]phenyl]butyric acid (J. Org. Chem. 26, 1554, (1961)) with N-hydroxysuccinimide and N-morpholinoethylisonitrile, 4-[2-[bis(2-chloroethyl)amino]phenyl]butyric acid N-hydroxysuccinimido ester is prepared. Said N-hydroxysuccinimido ester is reacted with 4-aminobutane-1,1-diphosphonic acid tetraethyl ester, according to the procedure described in Example 10, to give N-{4-[2-[bis(2-chloroethyl)amino]phenyl]butyroyl}-4-aminobutane-1,1-diphosphonic acid tetraethyl ester, which is reacted with iodotrimethylsilane, following the procedure described in Example 11, to obtain N-{4-[2-[bis(2-chloroethyl)amino]phenyl]butyroyl}-4-aminobutane-1,1-diphosphonic acid disodium salt.

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