Palladium (0)-catalysed arylations using pyrrole and indole 2-boronic acids
A versatile synthesis of 2-arylpyrroles and 2-arylindoles is described based on the use of either N-(Boc) pyrrole-2-boronic acid or N-(Boc) indole-2-boronic acid as components for Suzuki coupling.
Johnson, Christopher N.,Stemp, Geoffrey,Anand, Neel,Stephen, Susanna C.,Gallagher, Timothy
p. 1025 - 1027
(2007/10/03)
2-[(substituted)phenyl]-5-[1-(2-phenylazacycloheptyl) methyl]-1H-pyrroles with high affinity and selectivity for the dopamine D3 receptor
A series of 2-[(substituted)phenyl]-5-[1-(2-phenylazacycloheptyl)methyl]-1H-pyrroles (8 - 15) has been prepared to investigate the effect on affinity and selectivity for the dopamine D3 receptor of modifying the substituent in the phenyl ring at the 2-position of the pyrrole. Sulfonate 7 and sulfonamides 12, 14, 15 were shown to have high affinities (pKi's 8.0 - 8.7) and selectivities (100 - 150-fold) for the D3 over the D2 receptor.
Bolton, David,Boyfield, Izzy,Coldwell, Martyn C.,Hadley, Michael S.,Johns, Amanda,Johnson, Christopher N.,Markwell, Roger E.,Nash, David J.,Riley, Graham J.,Scott, Emma E.,Smith, Stephen A.,Stemp, Geoffrey,Wadsworth, Harry J.,Watts, Eric A.
p. 485 - 488
(2007/10/03)
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