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. 2015 May 14;127(27):8022–8025. doi: 10.1002/ange.201500250

Scheme 1.

Scheme 1

Synthesis of 2′‐deoxy‐2′‐difluoro‐5‐ethynyluridine (dF‐EdU, 3). a) Isopentyl nitrite, 0.1 N HCl, 70 °C, overnight; b) Ce(NH4)2(NO3)6, I2, HOAc, 80 °C, 2 h; c) ethynyltrimethylsilane, Pd(PPh3)2Cl2, CuI, Et3N, DMF, RT, 60 min; d) NaOH/H2O/MeOH, rt, 15 min. DMF=dimethylformamide.