3-Aminobicyclo[1.1.1]pentane-1-carboxylic Acid Derivatives: Synthesis and Incorporation into Peptides

Abstract 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 γ‐aminobutyric acid have been incorporated into linear and cyclic peptides using solution chemistry and solid‐phase techniques. (© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004)