Journal of labelled compounds and radiopharmaceuticals p. 635 - 643 (2005)
Update date:2022-08-10
Topics:
Lacan, Goran
Kesner, Amanda L.
Gangloff, Anne
Zheng, Lei
Czernin, Johannes
Melega, William P.
Silverman, Daniel H. S.
A fluorine-18 labeled analog of the widely used chemotherapeutic agent cyclophosphamide was synthesized as a tracer for prognostic imaging with positron emission tomography. 2-[(2-Chloro-2′-[18F]fluoroethyl) amino]-2H-1,3,2-oxazaphosphorinane-2-oxide (18F- fluorocyclophosphamide), was prepared by direct halogen exchange reaction from the parent cyclophosphamide. In small-scale syntheses, radiochemical yields of up to 4.9% and specific activities of 960 Ci/mmol were achieved in a total synthesis time of 60-75 min. The [18F]-labeled cyclophosphamide analog with radioactive purity >99% and chemical purity >96% was suitable for in vivo (microPET imaging) and ex vivo studies of a murine model of human breast tumors. Copyright
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