RADIOLABELED NUCLEOSIDE ANALOGUE, AND PREPARATION METHOD AND USE THEREOF

摘要

A radiolabeled nucleoside analogue is provided, which includes radioactive iodine 123I/131I, and a nucleoside analogue selected from a group consisting of cytidine, thymidine, uridine, and a derivative thereof. A method for preparing the radiolabeled nucleoside analogue, and a use thereof are further provided. The nucleoside analogue, prepared through the preparation method with a short synthesis time and a high radiochemical yield, has a long in vivo physiological half life and a high stability in serum, and, as a radiopharmaceutical composition, is useful in development of tumor proliferation diagnosis or therapy prognosis evaluation, and further assists in observation of long-time in vivo metabolism of a drug.

主权项

1. A method for preparing a radiolabeled nucleoside analogue, comprising:
(a) preparing a labeling precursor comprising a 5-tributylstannyl-2′-pyrimidine derivative, wherein the pyrimidine derivative in the labeling precursor is selected from a group consisting of a cytidine, a thymidine, a uridine, and a derivative thereof; (b) iododestannylating the labeling precursor with a radionuclide under an oxidation condition to obtain a radioactive iodine labeled crude product, wherein the radioactive iodine comprises a 123I and a 131I; and (c) purifying the radioactive iodine labeled crude product by directly cooling and solidifying with a liquid nitrogen in a vacuum system provided with an active carbon adsorbent so as to obtain the radiolabeled nucleoside analogue as a freezing dried powder merely containing a [123/131I]ICdR and a trace CdR.