221689-04-9Relevant academic research and scientific papers
C-14 labelling of NVP RAD001 - A new rapamycin derivative
Moenius,Voges,Mahnke,Burtscher,Metz,Guenat
, p. 29 - 41 (1999)
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.
