Technique for rapid peptide coupling

Details Technique for rapid peptide coupling Technique for rapid peptide coupling

C - Chemistry, Metallurgy

07

K

260/296, 260/316

C07K 1/08 (2006.01) C07D 207/46 (2006.01) C07D 209/48 (2006.01) C07D 213/89 (2006.01) C07D 249/18 (2006.01) C07D 253/06 (2006.01) C07D 253/08 (2006.01) C07D 487/08 (2006.01) C07K 1/10 (2006.01)

Patent

CA 2020650

ABSTRACT The present invention is directed to a process for forming a peptide bond between a first AMINO ACID containing a free N-terminal amino group and an acylating N-terminal amino protected second AMINO ACID which comprises reacting under amide forming conditions said first AMINO ACID with said second AMINO ACID in the presence of a basic and catalytic effective amount of a mixture comprising a tertiary amine of the formula: Image and a N-hydroxy nitrogen containing heterocycle or the quaternary ammonium salt of said mixture, wherein R1, R2, and R3 are independently lower alkyl, or R1 and R2 together with the nitrogen to which they are attached form a heterocyclic ring.

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