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.
Claims11
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;
- agitating the amino acids and peptide with an inert gas;
- 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
- monitoring the temperature of the vessel;
- and
- moderating the applied power based upon the monitored temperature by spiking the microwave energy in large amounts for short lengths of time.
A process for accelerating the solid phase synthesis of peptides, and comprising:
- transferring a first protected common amino acid linked to a resin, both suspended in an appropriate solvent, to a reaction cell;
- pumping a deprotection solution into the reaction cell;
- applying microwave energy to the first amino acid, the resin, and the solvent in the reaction cell;
- withdrawing the deprotection solution from the reaction cell, leaving the deprotected first common amino acid linked to the resin;
- washing the resin with a volume of an appropriate wash solvent that is substantially the same volume as the resin in the reaction cell;
- removing the wash solvent from the reaction cell;
- and
- thereafter adding a second deprotected common amino acid to the reaction cell along with an activating solution.
Dependencies are inferred from the claim text.