MICROWAVE-ASSISTED PEPTIDE SYNTHESIS

摘要

An instrument and method for accelerating the solid phase synthesis of peptides are disclosed. The method includes the steps of deprotecting a protected first amino acid linked to a solid phase resin by admixing the protected linked acid with a deprotecting solution in a microwave transparent vessel while irradiating the admixed acid and solution with microwaves, activating a second amino acid, coupling the second amino acid to the first acid while irradiating the composition in the same vessel with microwaves, and cleaving the linked peptide from the solid phase resin by admixing the linked peptide with a cleaving composition in the same vessel while irradiating the composition with microwaves.

主权项

1. A process for accelerating the solid phase synthesis of peptides, and comprising:
deprotecting the alpha-amino group of a first amino acid protected with a composition selected from the group consisting of N{acute over (α)}-9-fluorenylmethyloxycarbonyl (Fmoc) and N{acute over (α)}-t-butoxycarbonyl (Boc) and linked to solid phase resin particles by admixing the protected linked acid with a deprotecting solution in a microwave transparent vessel while irradiating the admixed acid and solution with microwaves; activating a second amino acid; coupling the second amino acid to the first acid while irradiating the composition in the same vessel with microwaves; agitating the amino acids and peptide with an inert gas; and successively deprotecting, and coupling a plurality of amino acids into a peptide in the same microwave transparent vessel without removing the peptide from the same vessel between cycles.