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

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Retrosynthesis <strong>of</strong> ApomorphineHOHOFGIA BN CH3C *MeODMeO(R/S)-[6a- 14 C]Apomorphine dimethyl ether*= 14 CRING CFORMATIONPschorrcouplingMeOADOMeBN*NO 2CH 3Bischler-NapieralskicyclodehydrationRING BFORMATIONMeOMeONO 2D*ON HATetrahydro[ 14 C]isoquinolineN-[carboxyl- 14 C]Acetamide
Synthesis <strong>of</strong> N-[carboxyl- 14 C]acetamideK 14 CN55mCi/mmolNO 2MeODMeO(COCl) 2DMFMeOMeOClNO 2D*OClMeOMeOANO 290% 86%86%(2 steps)NOacid2* hydrolysis MeOCN*OMeONONH 2H2 MeO* NDOMeOOHN-[carboxyl- 14 C]AcetamideARadiochemical yield = 67%
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 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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