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Transmetalation Methods for the Synthesis of PET and SPECT Imaging Agents

机译:PET和SPECT显像剂合成的重金属化方法

摘要

A process for the preparation of a radionuclide imaging agent includes providing an imaging agent including a chelated place-holder metal; loading the imaging agent onto an acid stable stationary phase; replacing the chelated place-holder metal of the imaging agent loaded on the stationary phase with a replacement radioactive metal under mild reaction conditions; and eluting the imaging agent including the chelated replacement radioactive metal from the stationary phase to provide a radionuclide imaging agent suitable for positron emission tomography (PET) or single-photon emission computed tomography (SPECT). The imaging agent can include a targeting agent that is directly conjugated to the imaging agent or by means of a linker. The process may also apply to other metals that are non-radioactive but used as diluent metals or other metals that are strongly bound to DOTA.
机译:一种制备放射性核素显像剂的方法,包括提供一种包含螯合的占位金属的显像剂。将显像剂加载到酸稳定的固定相上;在温和的反应条件下,用替代的放射性金属代替固定在固定相上的显像剂的螯合的占位金属;从固定相洗脱包含螯合的替代放射性金属的显像剂,以提供适合于正电子发射断层摄影(PET)或单光子发射计算机断层摄影(SPECT)的放射性核素成像剂。显像剂可包括直接与显像剂或通过接头偶联的靶向剂。该方法还可适用于非放射性但用作稀释金属的其他金属或与DOTA牢固结合的其他金属。

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