STABLE ISOLATED SYMMETRICAL ANHYDRIDES OF Nα‐9‐FLUORENYLMETHYLOXYCARBONYLAMINO ACIDS IN SOLID‐PHASE PEPTIDE SYNTHESIS:

Abstract
The synthesis and isolation of symmetrical anhydrides of Nα‐9‐fluorenylmethyloxycarbonyl (Fmoc) amino acids using water soluble carbodiimide is described. These compounds were used in a solid phase peptide synthesis of methionine‐enkephalin on a p‐benzyloxybenzyl ester polystyrene 1% divinylbenzene resin support. Homogeneous free pentapeptide was obtained in 42% overall yield. The Fmoc amino acid symmetrical anhydrides were stable during prolonged storage (2 years at 0°) and offer advantages over present “Fmoc solid phase” methods which use anhydrides formed in situ.

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