Palladium catalysts medicinal chemistry

An asymmetric synthesis of prolino-homotryptophane was accomplished via amino-zinc-ene-enolate cyclization followed by transmetalation of the cyclic zinc intermediate with indolyliodide. The use of palladium catalyst derived from [t-Bu3PH] BF4 was required to avoid the undesired P-hydride elimination. The resulting proline chimeras are useful tools for medicinal chemistry and/or biological applications. 

---