Synthesis of new substrates for near-infrared bioluminescence imaging

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In vivo molecular imaging that enables non-invasive observation of molecule of interest in organisms is a valuable technique to promote life science and drug discovery. In particular, the methods using near-IR luminescence have been aggressively developed in recent years. In order to develop a near-IR bioluminescence system based on coelenterazine (CTZ)-utilizing luciferase, we have established a concise synthetic method of v-CTZ, an analog that is known to show red-shifted light emission applicable to in vivo molecular imaging. The ten-step synthetic route of v-CTZ includes three consecutive regioselective cross-coupling reactions and ring closing metathesis as key reactions, which is suitable for preparing various analogs. We also synthesized C2-CF3-analog of v-CTZ, cf3-v-CTZ, and showed that it also serves as a good substrate for Renilla luciferases with increased stability.