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