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Table 5 Synthesis of 5-alkynyl pyrimidine analogues 50-52

From: Heck and Sonogashira couplings in aqueous media – application to unprotected nucleosides and nucleotides

Entry R 1 R 2 Starting Material R Product Yield (%)
1 OH H 1 50 95a
2 NH2 PO3H2 13 51 73b
3 NH2 P3O9H4 14 52 50c
  1. aPd(0) (10 mol%), ( 3 eq), NEt3 (2 eq), CuI (0.2 eq), CH3CN/H2O (1:1), 4 h.bPd(0) (20 mol%), ( 10 eq), NEt3 (10 eq), CuI (0.3 eq), CH3CN/H2O (1:1), 3 h. cPd(0) (20 mol%), (1.25 eq), NEt3 (10 eq), CuI (0.3 eq), CH3CN/H2O (1:1), 3 h.