Electric Literature of C9H10O2In 2021 ,《Metallaphotoredox aryl and alkyl radiomethylation for PET ligand discovery》 appeared in Nature (London, United Kingdom). The author of the article were Pipal, Robert W.; Stout, Kenneth T.; Musacchio, Patricia Z.; Ren, Sumei; Graham, Thomas J. A.; Verhoog, Stefan; Gantert, Liza; Lohith, Talakad G.; Schmitz, Alexander; Lee, Hsiaoju S.; Hesk, David; Hostetler, Eric D.; Davies, Ian W.; MacMillan, David W. C.. The article conveys some information:
Positron emission tomog. (PET) radioligands (radioactively labeled tracer compounds) are extremely useful for in vivo characterization of central nervous system drug candidates, neurodegenerative diseases and numerous oncol. targets1. Both tritium and carbon-11 radioisotopologues are generally necessary for in vitro and in vivo characterization of radioligands2, yet there exist few radiolabelling protocols for the synthesis of either, inhibiting the development of PET radioligands. The synthesis of such radioligands also needs to be very rapid owing to the short half-life of carbon-11. Here we report a versatile and rapid metallaphotoredox-catalyzed method for late-stage installation of both tritium and carbon-11 into the desired compounds via methylation of pharmaceutical precursors bearing aryl and alkyl bromides. Me groups are among the most prevalent structural elements found in bioactive mols., and so this synthetic approach simplifies the discovery of radioligands. To demonstrate the breadth of applicability of this technique, we perform rapid synthesis of 20 tritiated and 10 carbon-11-labeled complex pharmaceuticals and PET radioligands, including a one-step radiosynthesis of the clin. used compounds [11C]UCB-J and [11C]PHNO. We further outline the direct utility of this protocol for preclin. PET imaging and its translation to automated radiosynthesis for routine radiotracer production in human clin. imaging. We also demonstrate this protocol for the installation of other diverse and pharmaceutically useful isotopes, including carbon-14, carbon-13 and deuterium. In the experimental materials used by the author, we found 2-(Benzyloxy)acetaldehyde(cas: 60656-87-3Electric Literature of C9H10O2)
2-(Benzyloxy)acetaldehyde(cas: 60656-87-3) is a non-natural aldehyde. It undergoes enantioselective Mukaiyama aldol reaction with silylketene acetal nucleophiles in the presence of C2-symmetric bis(oxazolinyl)pyridine Cu(II) complex (catalyst).Electric Literature of C9H10O2
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Ether | (C2H5)2O – PubChem