ORGN 10 |
| We have developed a Pd(0)-catalyzed, Cu(I)-mediated cross coupling of boronic acids with cyclic thioamide or thiourea fragments under neutral conditions. These microwave-assisted transformations are related to the Liebeskind-Srogl reaction and provide carbon-carbon bond formation in a very efficient and rapid way. In the absence of Pd(0), carbon-sulfur cross coupling is observed. The mechanism of both processes will be discussed, and an application toward the synthesis Bay 41-4109, a highly potent non-nucelosidic inhibitor of hepatitis B virus replication, outlined. |
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Metal-Mediated Reactions and Syntheses
8:00 AM-12:00 PM, Sunday, 10 September 2006 Moscone Center -- Room 134, Oral
Division of Organic Chemistry |