[F:1][C:2]1[N:10]=[C:9]2[C:5]([NH:6][CH:7]=[N:8]2)=[C:4]([Cl:11])[N:3]=1.[C:12]1(P(C2C=CC=CC=2)C2C=CC=CC=2)[CH:17]=CC=C[CH:13]=1.CC(O)C.N(C(OCC)=O)=NC(OCC)=O>O1CCCC1>[F:1][C:2]1[N:10]=[C:9]2[C:5]([N:6]=[CH:7][N:8]2[CH:12]([CH3:17])[CH3:13])=[C:4]([Cl:11])[N:3]=1Anhydrous tetrahydrofuran (60 mL) is added to a flame-dried flask under N2 containing 2-fluoro-6-chloropurine (1.8 g, 10.4 mmol) and triphenylphosphine (6 g, 20.8 mmol). To this anhydrous 2-propanol (1.6 ml, 20.8 mmol) is added, and the mixture is then cooled to −10° C. After dropwise addition of 40% (W/V) diethyl azodicarboxylate in tetrahydrofuran (9 ml, 20.8 mmol), the mixture is warmed gradually to room temperature. After 18 h, the reaction mixture is quenched with 1 ml of water and the solvent is removed in vacuo. The resulting yellow oil is purified by column chromatography. The resulting solid is triturated with methanol (to remove the diethyl hydrazine-N,N′-dicarboxylate ester by-products) to yield 1.1 g (49%) as a white solid.
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