Synthesis of azapeptides from hindered amines leading to novel growth hormone secretagogues

Article abstract of DOI:10.1016/S0040-4039(99)01888-2

Preparations of aza analogues of known potent growth hormone secretagogues (GHS) were unsuccessful using known methods for preparation of azapeptides when hindered amines were employed. We now report a coupling method using bispentafluorophenylcarbonate as a 'balanced reactivity' phosgene equivalent to solve these problems.