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

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Bischler-Napieralski CyclodehydrationMeOMeONO 2D*OHNAP 2O 5/POCl 3TolueneMeOMeONO 2ND *OPimineAN-[carboxyl- 14 C]AcetamideMeOMeONO 2D*N +-OPAnitrilium saltRING BFORMATIONA*BN +ClHbasic work upA*BNMeODOMeNO 2MeODNO 2OMeDihydro[ 14 C]isoquinolineRadiochemical yield = 43%
N-Methylation Reduction StepMeOOMeNN +CH 3I/THFNO 2* * *I -NaBH 4/EtOHCH 3MeO NO MeO2OMeOMeNNO 2CH 3Dihydro[ 14 C]isoquinoline [ 14 C]Methiodide Tetrahydro[ 14 C]isoquinolineRadiochemical yield = 77%Bischler-NapieralskiEndocyclic Product
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 16 and 17: S L Kitson, S J Jones et al. J Labe
Page 18 and 19: Aporphine skeleton‘naturally occu
Page 20 and 21: Retrosynthesis of ApomorphineHOHOFG
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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