Microwave-assisted peptide synthesis
AssigneeCEM Corporation
InventorsJonathan McKinnon Collins, Joseph Joshua Lambert, Michael John Collins
Life of this patent
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Abstract
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.
Claims27
A process for the solid phase synthesis of peptides, which comprises:
- (a) transferring solid phase resin particles between a resin source external to a single microwave transparent vessel and into the microwave transparent vessel;
- (b) deprotecting a first amino acid linked to the solid phase resin particles by removing protective chemical groups from the first acid;
- (c) activating chemical groups on a second amino acid to prepare the second amino acid for coupling with the first amino acid;
- (d) coupling the activated second amino acid to the deprotected first amino acid to form a peptide from the first and second amino acids;
- (e) accelerating at least the deprotecting and coupling steps by applying microwave energy during the deprotecting, and coupling steps;
- and
- (f) successively deprotecting, and coupling a plurality of amino acids into a peptide in the single microwave transparent vessel without removing the peptide from the single vessel between cycles.
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 Na-9-fluorenylmethyloxycarbonyl (Fmoc) and Na-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;
- 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.
Dependencies are inferred from the claim text.