Abstract
AbstractAlkene 3, a TBS‐ and Cbz‐protected derivative of vinylglycinol, safely available from methionine, undergoes efficient Heck coupling reactions in high yields. The resulting products can be converted into enantiopure α‐amino acids with aromatic and heteroaromatic side‐chains. Compound 6a, a brightly fluorescent Fmoc‐protected pyrene amino acid is of special interest. Tripeptide 8a, composed of this building block and two arginines, binds to TAR, an RNA element regulating transcriptional efficiency in HIV, with a Kd value of 50 nM. This compound also inhibits a coupled cell‐free transcription‐translation assay (IC50 = 40 μM) and shows pronounced antibacterial activity against B. subtilis. (© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2008)
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