BOP reagent for solid phase peptide synthesis

Details BOP reagent for solid phase peptide synthesis BOP reagent for solid phase peptide synthesis

1987-04-30

1989-12-19

Kight, John

Synthetic resins or natural rubbers -- part of the class 520 ser

Synthetic resins

Mixing of two or more solid polymers; mixing of solid...

530333, 530334, A61K 3743, C07K 710

Patent

active

048883859

ABSTRACT:
A novel method of activation of a protected amino acid using Benzotriazolyloxytris(dimethylamino)phosphonium Hexafluorophosphate (BOP) as an activator for solid phase peptide synthesis is provided. Hydroxybenzotriazole is included in preferred embodiments. An intermediate acyloxyphosphonium salt is formed from the protected amino acid and the BOP which immediately reacts with HOBt to form an ester without formation of the less reactive symmetrical anhydride. A tertiary or quaternary substituted nitrogen compound must be used to produce a carboxylate of the protected amino acids as it also functions to increase their solubility.

REFERENCES:
patent: 4581168 (1986-04-01), Diaz et al.
patent: 4636490 (1987-01-01), Martinez et al.

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