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The 1-amino-2-hydroxybicyclo[2.2.1]heptane-7-carboxylic acid derivatives 1-3 have been synthesized, the pivotal step being the use of an acyl nitrene-insertion reaction to introduce nitrogen functionality into the corresponding hydroxy ester. The analogues each mimic a distorted peptide ground state as well as the transition state for peptide bond hydrolysis. To enhance the immune response and to...