In the past years the research directed toward protease-catalysed synthesis of small therapeutic peptides and oligopeptides received increasing attention. Obvious advantages of enzymatic synthesis over chemical approaches are the minimal protection required, the virtual absence of undesired side reactions and the easy separation of the products, features that make enzymatic processes really appealing, also from an industrial point of view. However, this approach has still not been thoroughly explored. Recently, we published the protease-catalysed selective deprotection of the C-terminal tert-butyl esters of peptides [1]. In this paper, we present recent developments by our groups in new synthetic applications for the modification of the carboxy-terminus of peptides, such as the C-terminal amidation and the synthesis of various esters by transesterification.
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