Premixed dry reagent containing a protected amino acid and an ac

Details Premixed dry reagent containing a protected amino acid and an ac Premixed dry reagent containing a protected amino acid and an ac

1990-09-14

1991-11-12

Schain, Howard E.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Synthesis of peptides

530333, 530335, C07K 106, C07K 100

Patent

active

050649400

ABSTRACT:
A novel and convenient process is described for providing protected amino acids and activating agents for solid phase synthesis which drastically reduces the capital costs of equipment required for the preparation of peptides. The two normally very reactive reagents, when mixed as anhydrous powders are shelf stable and yet form an active compound rapidly when mixed together in solution. This invention presents a method for combining these highly reactive dry solids in a manner which makes them unreactive and shelf stable at room temperature for extended periods of time. Once the solids are dissolved in solvent, a highly reactive amino acid ester that can readily be used in solid phase peptide synthesis is formed. This method of delivery of reagents to an automated peptide synthesizer allowers a very simplified instrument to be constructed using fewer and less expensive components and significantly reducing the associated software required.

REFERENCES:
patent: 4888385 (1989-12-01), Hudson
patent: 4965343 (1990-10-01), Felix et al.
Nguyen and Castro, Peptide Chemistry 1987: T. Shiba & S. Sakakibara (ed.), 1988.
Bodanszky, Principles of Peptide Synthesis, Springer-Verlag, 1984, pp. 238-239.
D. Hudson, J. Org. Chem. 53, 617-624 (1988).

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