3-aminobicyclo[1.1.1]pentane-1-carboxylic acid derivatives:: Synthesis and incorporation into peptides

We have developed an efficient synthesis of derivatives of 3-aminobicyclo[1.1.1]pentane-1-carboxylic acid (7, 8, 9, and 10) starting from [1.1.1]propellane (3). These rigid analogues of gamma-aminobutyric acid have been incorporated into linear and cyclic peptides using solution chemistry and solid-phase techniques. ((C) Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004).