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2-{[(1S)-1-Methylbutyl]oxy}-9-(tetrahydro-2H-pyran-2-yl)-9H-purin-6-amine (1050 g) was dissolved in DCM (10.5 L) to give a yellow/orange solution which was cooled to 0° C. N-Bromosuccinimide (922 g, 1.5 eq) was charged in 3 equal portions 20 mins. apart and the resultant reaction mixture was stirred at 0-5° C. for 4 hours. The reaction was then quenched by addition of a solution of 500 g sodium thiosulfate pentahydrate in 5.0 L water. The resultant biphase was mixed thoroughly at 20° C. and then the phases were separated. The organics were washed again with a solution of 500 g sodium thiosulfate pentahydrate in 5.0 L water then 500 g dipotassium phosphate in 5.0 L water and finally with 5.0 L water. The organic phase was dried over magnesium sulfate (822 g) and evaporated on a rotary evaporator until foaming became prohibitive. The mixture was then solvent-exchanged into methanol by repeated addition and removal of methanol until sufficient DCM had been removed (as confirmed by NMR). The product was afforded as a red/brown gum containing entrained solvent (1.28 kg corrected for solvent, 96% theoretical yield).

1. customto give a yellow/orange solution which
2. customapart and the resultant reaction mixture
3. customThe reaction was then quenched by addition of a solution of 500 g sodium thiosulfate pentahydrate in 5.0 L water
4. additionThe resultant biphase was mixed thoroughly at 20° C.
5. customthe phases were separated
6. washThe organics were washed again with a solution of 500 g sodium thiosulfate pentahydrate in 5.0 L water
7. dry with materialThe organic phase was dried over magnesium sulfate (822 g)
8. customevaporated on a rotary evaporator
9. additionaddition and removal of methanol until sufficient DCM
10. customhad been removed (as confirmed by NMR)
11. customThe product was afforded as a red/brown gum
12. additioncontaining entrained
13. customsolvent (1.28 kg corrected for solvent, 96% theoretical yield)