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. Author manuscript; available in PMC: 2015 Sep 12.
Published in final edited form as: Eur J Med Chem. 2014 Jul 16;84:476–490. doi: 10.1016/j.ejmech.2014.07.050

Table 1.

Optimization of the Suzuki coupling of compound 2.

Compounds Pd-source Ligand Base Solvents Yields (%)
3 Pd[P(Ph)3]4 K2CO3 THF/MeOH 4
3 Pd(OAc)2 XPhosa K3PO4 THF/MeOH 44
4 Pd[P(Ph)3]4 K2CO3 THF/MeOH 12
4 Pd(OAc)2 Xphosa K3PO4 THF/MeOH 53
5 Pd[P(Ph)3]4 K2CO3 THF/MeOH 8
5 Pd(OAc)2 Xphosa K3PO4 THF/MeOH 61
6 Pd[P(Ph)3]4 K2CO3 THF/MeOH 4
6 Pd(OAc)2 XPhosa K3PO4 THF/MeOH 41
7 Pd[P(Ph)3]4 K2CO3 THF/MeOH 9
7 Pd(OAc)2 Xphosa K3PO4 THF/MeOH 55
8 Pd[P(Ph)3]4 K2CO3 THF/MeOH 4
8 Pd(OAc)2 XPhosa K3PO4 THF/MeOH 42
9 Pd[P(Ph)3]4 K2CO3 THF/MeOH 7
9 Pd(OAc)2 Xphosa K3PO4 THF/MeOH 57
a

XPhos: (2-biphenylyl)-dicyclohexyl-phosphine.