Table 3. Screening of different catalysts, substrates and reaction conditions for Suzuki and Sonogashira “on-DNA” cross-couplings.
| ||||
---|---|---|---|---|
Pd(II) Source |
Cu(II) Source |
Monitored after | Temp. | Eq. of Pd [a] |
Pd(Oac)2 | Cu(Oac)2 | 10 mins | 50 °C | 0.2 |
PdCl2 | Cu(SO4)2 | 1 hour | 60 °C | 0.5 |
PdCl2(PPh3)2 | Cu(Otf)2 | 2 hours | 65 °C | 1.0 |
[PdCl(allyl)]2 | Cu(Oac)2L | 4 hours | 70 °C | 1.5 |
Copper-free | 24 hours | 2.0 | ||
4.0 |
Equivalents with respect to DNA - aryl halide conjugate (3).