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Synthesis of "No Carrier Added" 1,3-Bis-(2-chloroethyl)nitrosourea (BCNU)

Montreal Neurological Institute, McGill University, 3801 University Street, Montreal, Quebec, H3A 2B4

Correspondence: For reprints contact: Dr. M. Diksic, Medical Cyclotron Facility, Montreal Neurological Institute, McGill University, 3801 University Street, Montreal, Quebec, H3A 2B4.

ABSTRACT

A chemotherapeutic agent, C-11-labeled BCNU, has been prepared by nitrosation of C-11-labeled BCU, which was synthesized by reacting C-11-labeled phosgene with ethylenimine. Two methods of nitrosation are outlined and the results of both are discussed. The specific activity of C-11 BCNU was about 85 Ci/mmole at the end of bombardment and 30 Ci/mmole at the time of administration. Chemical and radiochemical purity of the final material was at least 98%.