Synthetic Strategies for 14C Labelling of Drug Molecules Dr ... - Almac

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S L Kitson, S J Jones et al. J Label Compd. Radiopharm 2010, 53, 140-146NaOHEtOHSTEP 368%F 3CClNH 2O* OMOM[ 14 C]-8OOLiHMDS / THF-20 o C to -10 o CSTEP 4F 3CClHN*[ 14 C]-9OOHOMOMIPA, HCl45 o CColumn ChromatographyF 3CClHN*OOHOHOverall Radiochemical Yield ~ 30%STEP 563%[ 14 C]XEN-D0401* = Carbon-14 label
Key Step: A one pot construction <strong>of</strong> the quinolin-2-onering under strong baseF 3CClHN HO*O[ 14 C]-8OLiHMDS (2eqv)OOcondensationF 3CClOLiOHNLiO*OdianionOLiHMDSF 3CClOLiO-NLiO*OOcyclisationF 3CLiN O*LiOOCltrianionOLiOH 2OF 3CHOHN*OHOOHOLiOH-H 2OdehydrationF 3CClHN*OOOHOCl[ 14 C]-9
Page 4 and 5: Introduction to 14 Ccpres/v1b/ca/19
Page 6 and 7: 14C Starting Materials
Page 8 and 9: 14C Radiotracer• In pharmaceutica
Page 10 and 11: Target: [ 14 C]XEN-D0401• XEN-D04
Page 12 and 13: Generation of ‘Dry’ 14 CO 2HIGH
Page 14 and 15: O-MethylationHO*OOOK 2CO 3/ Acetone
Page 18 and 19: Aporphine skeleton‘naturally occu
Page 20 and 21: Retrosynthesis of ApomorphineHOHOFG
Page 22 and 23: Bischler-Napieralski Cyclodehydrati
Page 24 and 25: Reduction-Pschorr CouplingNCH 3N*CH
Page 26 and 27: (R)-(-)-[6a- 14 C]ApomorphineMeO*N
Page 28 and 29: Target: [methyl- 14 C]Combretastati
Page 30 and 31: [ 14 C]AcetylenesOH14COTarget: [5-
Page 32 and 33: 14C Acetylene SynthesisBrOHOp-TsOHE
Page 34 and 35: 14C SynthesisOHOMOMOMOMNaH/DMFn-BuL
Page 36 and 37: ConclusionWhen designing a 14 C lab

Synthetic Strategies for 14C Labelling of Drug Molecules Dr ... - Almac

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