Bop reagent for solid phase peptide synthesis

Details Bop reagent for solid phase peptide synthesis Bop reagent for solid phase peptide synthesis

C - Chemistry, Metallurgy

07

K

31/1, 530/1.1

C07K 1/10 (2006.01) B01J 19/00 (2006.01) C07K 1/04 (2006.01) C07K 1/06 (2006.01) C07K 1/08 (2006.01)

Patent

CA 1311332

ABSTRACT OF THE DISCLOSURE A novel method of activation of a protected amino acid using Benzotriazolyloxytris(dimethylamino)phosphonium Hexafluorophos- phate (BOP) as an activator for solid phase peptide synthesis is provided. Hydroxybenzotriazole is included in preferred embodi- ments. 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 guaternary substituted nitrogen compound must be uded to produce a carboxylate of the protected amino acids as it also functions to increase their solubility. -18-

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