| Popis: |
Tritium labeled isotopomers of (2S,3R)-3-[(2-carboxyethyl)thio]-3-[2-(8-phenyloctyl)phenyl]-2-hydroxypropionic acid (SK&F 104353) with high specific activity were prepared by catalytic tritiation of the corresponding halogenated and unsaturated precursors. These precursors were synthesized from their respective benzaldehydes using a core sequence (Darzens Condensation, epoxide opening and base-induced retroaldol reaction) to generate the required alpha-hydroxy propionic acid moiety. Upon tritiation, the halogenated substrate provided the dimethyl ester derivative having a specific activity of 55 Ci/mmol, while the unsaturated precursor led directly to [3H]SK&F 104353 with a specific activity of 138 Ci/mmole. |
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