a-Amino acids are {among|amongst} the {essential|important|crucial|vital|necessary|critical} chemical {building|developing|creating|constructing} blocks of life. These structures are embedded in {many|numerous|several|a lot of|quite a few|lots of} {small|little|tiny|modest|smaller|compact} molecule pharmaceuticals and {are the|would be the|will be the} {primary|main|major|principal|key} {components|elements} of peptide-based therapeutics and biologics. Isotopically labeled a-amino acids and their derivatives have widespread use in structural and mechanistic biochemistry, quantitative proteomics, absorption distribution metabolism and excretion (ADME) profiling, and as imaging agents in positron emission tomography (PET) {techniques|methods|strategies|tactics|approaches|procedures}. The preparation of carbon-labeled a-amino acids remains {difficult|tough|challenging|hard|tricky|complicated} and time consuming, with established {methods|techniques|strategies|approaches|procedures|solutions} involving label incorporation at an early stage of synthesis. This explains the {high|higher} {cost|price|expense} and scarcity of C-labeled {products|goods|items|merchandise|solutions} and presents {a major|a significant} challenge in 11C applications (11C t1/2 = 20 min). {Here|Right here} we report that {simple|easy|straightforward|basic|uncomplicated|very simple} aldehydes catalyze the isotopic carboxylate exchange of native a-amino acids with *CO2 (* = 14, 13, 11). Proteinogenic a-amino acids and {many|numerous|several|a lot of|quite a few|lots of} non-natural variants containing diverse functional groups undergo labeling. The reaction {likely|most likely|probably} proceeds {via|by way of|through|by means of} the trapping of *CO2 by imine-carboxylate intermediates to {generate|produce|create} aminomalonates {that are|which are|which can be|which might be|that happen to be} prone to monodecarboxylation. Tempering catalyst electrophilicity was {key|important|crucial|essential} to {preventing|stopping} irreversible aldehyde consumption. The pre-generation {of the|from the|in the|on the|with the|of your} imine carboxylate intermediate {allows|enables|permits|makes it possible for} for the {rapid|fast|speedy} and late-stage 11C-radiolabeling of a-amino acids {in the|within the|inside the} presence of 11CO2. 1,4-Dihydropyrazine-2,3-dithione web 1178566-52-3 Price PMID:24670464
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