Journal of labelled compounds and radiopharmaceuticals p. 29 - 41 (1999)
Update date:2022-08-05
Topics:
Moenius
Voges
Mahnke
Burtscher
Metz
Guenat
An optimized fermentation process is described for the carbon-14 labelling of rapamycin. It is characterized by good reproducibility, high radiochemical purity and excellent yields. L-[14C2]Pipecolic acid and (1R,3R,4R)-3,4-dihydroxy[1,7-14C2]cyclohexane carboxylic acid ([14C2]DHCCA) synthesized in an effective stereoselective approach proved to be highly suitable precursors for this purpose. In a final step [14C4]rapamycin was converted by selective 14C(40)-O-alkylation to [14C4]NVP RAD001, a highly interesting immunosuppressant.
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